Search

• Development of a detection method to operate from discrete photons to continuous photon input signals and automatically detects either of them. • Development of photon-counting methods using combined logic of pulse width and pulse potential amplitude. • Facilitates multichannel scaler application which offers a feature of a bin by bin photon count analysis of acquired larger bin size. • Better dynamic range compared to SR400 gated photon counter. A sensor like a photomultiplier tube (PMT) has shown many applications, particularly in the photon counting regime, where it generates discrete electrical pulses in response to the input photons. Commercially available photon counters used to count these pulses assuming the incident photons in the discrete form. In general, whenever two or more photons arrive concurrently, the photon counter record it as a single pulse and count it as single count. On the contrary, when continuous photons arrive, the discrete photon counting approach ceases to function, and a continuous capture technique is used to estimate the photons intensity. In this article, a photon-counting method based on a data acquisition card (DAQ Model: Agilent U1071A), which works in the discrete to continuous photon regime where the commercial photon counters stop counting is described. To facilitate the precise counting of the discrete and merged pulses, a program has been developed in LabVIEW incorporating the logic of pulse width and amplitude. The developed technique is tested for its functionality and compared with the commercially available photon counter SR400. The outcomes of the study indicate that the developed system is capable of operating from discrete photons to a continuous regime and has a better dynamic range than the SR400 gated photon counter. [ABSTRACT FROM AUTHOR]

This study analysed buffaloes from north-east India and compared their nuclear and mitochondrial DNA variations with buffaloes of mainland India, China, Mediterranean and South-East Asia. Microsatellite genotypes of 338 buffaloes including 210 from six north-east Indian buffalo populations and three mainland Indian breeds were analysed to evaluate their genetic structure and evolutionary relationships. Phylogenetic analysis and multidimensional scaling plot of pairwise FST revealed the clustering of all swamp-type buffaloes of north-east India with Lower Assamese (significantly hybrid type) buffaloes in one plane and all the mainland river buffaloes in another plane while the upper Assamese buffaloes being distinct from both these clusters. Analysis of mtDNA D-loop region of 530-bp length was performed on 345 sequences belonging to 23 buffalo populations from various geographical regions to establish the phylogeography of Indian water buffalo. The swamp buffaloes of northeast India clustered with both the lineages of Chinese swamp buffalo. Multidimensional scaling display of pairwise FST derived from mitochondrial DNA data showed clustering of upper Assamese, Chilika and Mediterranean buffaloes distinctly from all the other Indian buffalo populations. Median-joining network analysis further confirmed the distinctness and ancestral nature of these buffaloes. The study revealed north-east region of India forming part of the wider hybrid zone of water buffalo that may probably extend from north-east India to South-East Asia. [ABSTRACT FROM AUTHOR]

Radiation force balance approach is universally adopted and most widely used primary calibration method for total acoustic power radiated by an ultrasonic transducer. In this setup, the separation between the transducer and target (absorbing/reflecting) plays vital role in the overall measurement uncertainty of ultrasonic power due to attenuation of ultrasonic waves within the travel path. It becomes relatively more important at high frequencies as the ultrasonic attenuation is proportional to the square of frequency. Hence, the separation between the transducer and the target need to be measured with the best possible resolution and least uncertainty. In this article, two methods developed for transducer and target separation measurement have been described and compared. The first method uses displacement sensor in the feedback and controls stepper motor in micro stepping and adjust the separation with control program. It also uses the microbalance feedback approach to automatically detect the null (zero) distance. In the second approach, which does not use distance sensor in feedback and a triangle method is used to detect change in height. High torque stepper motor is used in micro-stepping mode to achieve best step resolution of one μm. Second method is free from error that cause due to electrical noise in sensor and has provision for backlash error correction. The article contains developmental details and functionalities of these methods. [ABSTRACT FROM AUTHOR]

Abstract: The exploration of candidate immune response genes in goat may be vital in improving further our understanding about the species specific response to pathogens specifically among the ruminants. In this study, approximately 3.7kb long genomic sequence of Toll-like receptor 5 (TLR5) covering the entire coding and 5′upstream regions of the gene, was characterized in the Indian goat breeds. Sequence analysis revealed a 2577-nucleotide long open reading frame (ORF) of goat TLR5, encoding 858 amino acids from single exon, similar to other ruminants. The domain structure analysis of goat TLR5 showed the presence of 13 leucine rich repeats (LRRs) in extracellular domain (amino acid position 1–634), single transmembrane domain (position 644–666), and a Toll/interleukin-1 receptor (position 692–837) in cytoplasmic domain, similar to other species. A total of 87 putative transcription factor binding sites were observed within the 5′ upstream region of TLR5 gene in goat, 106 in cattle, and 103 in buffalo. Sixteen polymorphic sites were observed in goat TLR5 gene, out of which 10 non-synonymous SNPs were in the functionally important regions. However, none of the amino acid substitutions was found to be potentially damaging to the structure and function of the receptor protein. Further, one of the SNPs in the transmembrane region was genotyped by a TETRA-ARMS PCR in 444 goats of nine breeds from different geographical regions and having different utilities. A significant variation in allelic frequencies was observed across the milch and other types of goat breeds. The comparative modeling of goat TLR5 followed by molecular dynamics simulation gave an insight into its 3D structural arrangements. The molecular docking of Salmonella flagellin and TLR5 dimer elucidated LRRNT (N-terminal) to LRR4 as the key flagellin binding domains region in goat TLR5. The study shows that, although being highly conserved among the ruminants, comparatively high variations in goat TLR5 might give an opportunity to host for recognizing the wider spectrum of pathogens. [Copyright &y& Elsevier]

L-Proline has been utilized as a novel and ecofriendly catalyst in ethanol medium for the Knoevenagel condensation of indole-3-carboxyaldehydes and their N-methyl derivatives 1(a–e) and 4(a–e) with the active methylene compound, ethyl cyanoacetate (2) to afford substituted (E)-ethyl 2-cyano-3-(1H-indol-3-yl)acrylates 3(a–e) and 5(a–e) respectively. These products were reacted with dimethyl sulfate in the presence of PEG-600 as an efficient and green solvent to afford the corresponding N-mthylated derivatives 5(a–e). These Knoevenagel products react with 5% NaOH, yielding (E)-3-(1H-indol-3-yl)acrylonitriles 6(a–e) and 7(a–e). [ABSTRACT FROM PUBLISHER]

Abstract: The synthesis of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives has been carried out using trifluoroacetic anhydride/phosphoric acid mediated C–C bond forming reaction as a key step. This method does not require the use of environmentally harmful AlCl3 or moisture sensitive acid chloride. A number of compounds containing the benzooxazinone moiety attached to a five-membered central heterocyclic ring was synthesized and tested for their anti-cancer properties in vitro against three cell lines e.g. A549 (lung), DLD-1 (colorectal adenocarcinoma) and MV4-11 (acute myeloid leukemia). Some of them showed anti-cancer activities along with a number of reference compounds tested. Few of them showed promising anti-leukemic properties. A brief Structure–Activity-Relationship study within the series is presented. An imidazole derivative 9c containing benzene ring with a para-CF3 group at C-2 position was identified as a potent anti-leukemic agent. [Copyright &y& Elsevier]

[image omitted] Reaction of arylmethyl/heteryl methyl zinc chloride (generated in situ from aryl methyl and heteryl methyl chloride and zinc metal) with aryl sulfonyl chlorides in tetrahydrofuran (THF) under mild conditions (i.e., at room temperature) furnishes the corresponding 1-(aryl sulfonyl)aryl/heteryl methanes in good yields. [ABSTRACT FROM AUTHOR]

A facile and eco-friendly methodology for the synthesis of N-alkyl/aralkyl derivatives of indole & indole-3-carboxyaldehydes mediated by polyethylene glycol as an efficient and green solvent is described. [ABSTRACT FROM AUTHOR]

Abstract: Anode made of multiwalled carbon nanotubes (MWNT) results in enhancement of exchange current density compared to graphite anode in a conventional alkaline water electrolysis cell. The hydrogen production rate with the nanotubes was measured to be ∼375lh−1 m−2 at pH∼14 which was nearly double of that obtained from traditional graphitic carbon electrodes at the same overpotential. This effect appears to be caused by defects on the nanotubes which reduces the energy barrier for the dissociation of OH− into oxygen at the anode. [Copyright &y& Elsevier]

Abstract: Monoamine Oxidase B interaction with known ligands was investigated using combined pharmacophore and structure based modeling approach. The docking results suggested that the pharmacophore and docking models are in good agreement and are used to identify the selective MAO-B inhibitors. The best model, Hypo2 consists of three pharmacophore features, i.e., one hydrogen bond acceptor, one hydrogen bond donor and one ring aromatic. The Hypo2 model was used to screen an in-house database of 80,000 molecules and have resulted in 5500 compounds. Docking studies were performed, subsequently, on the cluster representatives of 530 hits from 5500 compounds. Based on the structural novelty and selectivity index, we have suggested 15 selective MAO-B inhibitors for further synthesis and pharmacological screening. [Copyright &y& Elsevier]

Abstract: This paper deals with how the Hydrogen Energy may play a crucial role in taking care of the environmental scenario/climate change. The R&D efforts, at the Hydrogen Energy Center, Banaras Hindu University have been described and discussed to elucidate that hydrogen is the best option for taking care of the environmental/climate changes. All three important ingredients for hydrogen economy, i.e., production, storage and application of hydrogen have been dealt with. As regards hydrogen production, solar routes consisting of photoelectrochemical electrolysis of water have been described and discussed. Nanostructured TiO2 films used as photoanodes have been synthesized through hydrolysis of Ti[OCH(CH3)2]4. Modular designs of TiO2 photoelectrode-based PEC cells have been fabricated to get high hydrogen production rate (∼10.35lh−1 m−2). However, hydrogen storage is a key issue in the success and realization of hydrogen technology and economy. Metal hydrides are the promising candidates due to their safety advantage with high volume efficient storage capacity for on-board applications. As regards storage, we have discussed the storage of hydrogen in intermetallics as well as lightweight complex hydride systems. For intermetallic systems, we have dealt with material tailoring of LaNi5 through Fe substitution. The La(Nil − x Fe x )5 (x =0.16) has been found to yield a high storage capacity of ∼2.40wt%. We have also discussed how CNT admixing helps to improve the hydrogen desorption rate of NaAlH4. CNT (8mol%) admixed NaAlH4 is found to be optimum for faster desorption (∼3.3wt% H2 within 2h). From an applications point of view, we have focused on the use of hydrogen (stored in intermetallic La–Ni–Fe system) as fuel for Internal Combustion (IC) engine-based vehicular transport, particularly two and three-wheelers. It is shown that hydrogen used as a fuel is the most effective alternative fuel for circumventing climate change. [Copyright &y& Elsevier]

The title compound (5) has been prepared in one pot by refluxing 1-(1-alkyl/aralkyl-1H-benzimidazole-2-yl)-ethanone (1) with substituted o-phenylenediamine (2) in ethanol in the presence of iodine. Alternatively, 5 could also be prepared by treating 2-bromo-1-(1- alkyl/aralkyl-1H-benzimidazole-2-yl)-ethanone (3A) with 2 in refluxing ethanol. The formation of 5 from 1 and 2 probably occurs through the intermediacy of 3B (i.e., 3, X=I) and 4. [ABSTRACT FROM AUTHOR]

Abstract: A chiral selective, accurate and reproducible high-performance liquid chromatographic (HPLC) method was developed and validated for direct separation of individual enantiomers of torcetrapib (TTB) [(+)-TTB and (−)-TTB]. TTB enantiomers and IS were extracted from a small aliquot of plasma (100μL) by simple liquid–liquid extraction using acetonitrile as extraction solvent. The enantiomers were resolved on Chiralpak AD-H® (250mm×4.6mm, 5μm) with the mobile phase consisting of n-hexane:isopropyl alcohol (IPA) in the ratio of 95:5 (v/v). The eluate was monitored using an UV detector set at 254nm. Baseline separation of the TTB enantiomers and the internal standard (IS, DRL-17859), free from endogenous interferences was achieved. The resolution factor between the enantiomers was optimized and found to be not less than five. During method development, the IPA content in the mobile phase was optimized for separation of peaks of interest. Additionally, both flow rate and column temperature were optimized for an improved baseline separation of the enantiomers. Ratio of peak area of each enantiomer to IS was used for quantification of plasma samples. Nominal retention times of (+)-TTB, (−)-TTB and IS were 9.4, 13.8 and 17.5min, respectively. The standard curves for TTB enantiomers were linear (r 2 >0.999) in the concentration range 0.1–10μg/mL for each enantiomer. Absolute recovery, when compared to neat standards, was 88.7–90.0% for TTB enantiomers and 100% for IS from the hamster plasma. The lower limit of quantification (LLOQ) for each enantiomer of TTB was 0.1μg/mL. The inter-day precisions were in the range of 4.57–6.32 and 5.66–11.0% for (+)-TTB and (−)-TTB, respectively. The intra-day precisions were in the range of 1.60–7.36 and 2.76–13.6% for (+)-TTB and (−)-TTB, respectively. Accuracy in the measurement of quality control (QC) samples was in the range of 95.6–109% and 92.7–108% for (+)-TTB and (−)-TTB, respectively. Both enantiomers were stable in a series of stability studies, viz. bench-top (up to 12h), auto-sampler (up to 24h) and freeze/thaw cycles (n =3). Stability of TTB enantiomers was established in hamster plasma for 15 days at −80°C. The application of the assay to a pharmacokinetic study of (−)-TTB in hamsters is described. [Copyright &y& Elsevier]

Condensation of (1H-benzimidazole-2-yl)-acetonitrile 1 with aromatic aldehydes in 5% NaOH solution gave the corresponding 2-(1H-benzimidazole-2-yl)-3-aryl-acrylonitrile 2, which on treatment with NaBH4 in ethanol unexpectedly gave 2-(1H-benzimidazole-2-yl)-3-aryl-propionitrile 3 by the regiospecific reduction of the double bond. Shaking a solution of 2 with H2/Pd-C in methanol also gave 3. Reaction of 2 with DMS gave the corresponding N-methylated analogue 5, which also with NaBH4 gave 6, once again by the regiospecific reduction of the double bond as in the case of 1-demethylated analogue (i.e., 2). [ABSTRACT FROM AUTHOR]

Acetylation of 1H-2-(α-hydroxyalkyl/aryl)benzimidazoles 2 with Ac2O results in the regiospecific formation of O-acetoxy derivative 3, which on alkylation with alkylating agents in nonaqueous media under phase-transfer catalytic conditions affords N-alkyl derivatives 4. The latter, on hydrolysis in an aqueous basic medium, results in the title compounds 5 in good yields in high purity. Alternatively, 5 can also be obtained by reduction of 1-substituted-2-acetyl/benzoylbenzimidazoles 8 using NaBH4. [ABSTRACT FROM AUTHOR]

Condensation of o-phenylenediamine sulfate with cinnamic acids in refluxing ethylene glycol yielded the corresponding 2-styrylbenzimidazoles in excellent yields. [ABSTRACT FROM AUTHOR]

Blood pressure (BP) measurement is very important and crucial parameter for monitoring, controlling and treatment of human health conditions. Measurement of BP is performed using variety of instruments. Out of these, (i) mechanical or mercury manometers and (ii) oscillometric digital sphygmomanometers, are the most commonly used devices. Although, the international recommendations (OIML R16-2) for the automatic BP measuring instrument is available, there is no uniform international standard or method of calibration available. In this paper, a terse review of different types of BP measuring techniques and devices, commercially available is presented along with some related important historical developments. A concise and consolidated report of the several existing methods of BP device calibration being used at various National Metrology Institutes (NMIs) and other leading research groups is also included. This would open new lines for the future researchers to standardise a uniform and acceptable calibration method for these devices which is need of the hour. [ABSTRACT FROM AUTHOR]

On account of the high d.c. electric fields employed in the gas discharge tube plasmas, the electron temperature is much higher than the heavy particle temperature. Under such a non-thermal equilibrium, the propagation parameters for microwaves and radiowaves are considerably influenced by the d.c. electric field through the energy dependent electron collision frequency. As an example the cyclotron resonance of the extraordinary mode is suppressed and shifted by the hot electron effects. [ABSTRACT FROM AUTHOR]

The IT-SOFC candidate interconnect material ZMG232G10® was thermally pre-treated in air and in H 2 – 3% H 2 O to mitigate dual atmosphere corrosion. Bare and pre-treated steel samples were exposed to a dual atmosphere exposure condition (dry air/metal/4% H 2 – N 2 (bal.) + 3% H 2 O) for 500 h at 600 °C. Corrosion products and oxide morphology developed on the air-exposed surfaces were analyzed. Pre-treatments of the metal in oxidizing (air) and reducing (H 2 – 3% H 2 O) gas atmospheres provide improved passivation against dual atmosphere corrosion compared to bare steel. The uniform and iron-free oxide scale developed during the pre-treatment of alloy in the low pO 2 H 2 – 3% H 2 O gas atmosphere provides an effective diffusion barrier against the outward transport of cations and oxidation of iron observed under dual atmosphere conditions. • Pre-treatments suppress the formation of localized iron oxide nodules. • Low pO 2 pre-treatment promotes iron-free, columnar oxide scale resistant to breakdown. • Breakaway corrosion is caused by intrinsic chemical and mechanically induced failure of pre-treatment scales. [ABSTRACT FROM AUTHOR]

Fatty Acid Synthase ( FASN ) gene seems to be structurally and functionally different in bovines in view of their distinctive fatty acid synthesis process. Structural variation and differential expression of FASN gene is reported in buffalo ( Bubalus bubalis ), a bovine species close to cattle, in this study. Amino acid sequence and phylogenetic analysis of functionally important thioesterase (TE) domain of FASN revealed its conserved nature across mammals. Amino acid residues at TE domain, responsible for substrate binding and processing, were found to be invariant in all the mammalian species. A total of seven polymorphic nucleotide sites, including two in coding region of TE domain were identified across the 10 buffalo populations of riverine and swamp types. G and C alleles were found almost fixed at g18996 and g19056 loci, respectively in riverine buffaloes. Principal component analysis of three SNPs (g18433, g18996 and g19056) revealed distinct classification of riverine and swamp buffalo populations. Reverse Transcription-PCR amplification of mRNA corresponding to exon 8–10 region of buffalo FASN helped in identification of two transcript variants; one transcript of 565 nucleotides and another alternate transcript of 207 nucleotides, seems to have arisen through alternative splicing. Both the transcripts were found to be expressed in most of the vital tissues of buffalo with the highest expression in mammary gland. Semi-quantitative and real-time expression analysis across 13 different buffalo tissues revealed its highest expression in lactating mammary gland. When compared, expression of FASN was also found to be higher in liver, adipose and skeletal muscle of buffalo tissues, than cattle. However, the FASN expression was highest in adipose among the three tissues in both the species. Results indicate structural and functional distinctiveness of bovine FASN . Presence of alternate splicing in buffalo FASN also seems to be a unique phenomenon to the bovines, probably associated with mRNA based regulation of the biological functions of FASN in these species. [ABSTRACT FROM AUTHOR]

Environmental friendly syntheses of potential analgesic and antipyretic compounds, 2-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-N-(4-hydroxyphenyl)acetamide derivatives6a–6gand N-[(4-hydroxy-phenylcarbamoyl)-methyl]-phthalamic acid derivatives10a–10ghave been developed. Two synthetic routes (A and B) have been established for the preparation of6a–6g. In route A, 4-aminophenol2was reacted with chloroacetyl chloride3in a solution of potassium acetate and acetic acid to yield N-(4-hydroxyphenyl)-2-chloroacetamide4. The latter was reacted with imide compounds5a–5geither in triethanolamine as a green solvent or in solid phase in the presence of triethylbenzylammonium chloride and potassium iodide (KI) to yield6a–6g. Alternatively, in route B, the reaction of anhydrides7a–7gwith glycine8yielded the (1,3-dioxo-1,3-dihydroisoindol-2-yl)acetic acid derivatives9a–9gwhich on reaction with2either in triethnolamine and dicyclohexylcarbodiimide (DCC) as a dehydrating agent or in solid phase in the presence of DCC gave6a–6g. The latter were hydrolysed in 0.5N ethanolic potassium hydroxide (KOH) to afford10a–10g. [ABSTRACT FROM AUTHOR]

Both AF-2785 and gamendazole are experimental male oral contraceptives. The total syntheses of these two compounds are achieved in good yields. Supplemental materials are available for this article. Go to the publisher's online edition ofSynthetic Communications® to view the free supplemental file. [ABSTRACT FROM AUTHOR]

A general synthetic approach has been developed for the synthesis of a key intermediate (6) that can be elaborated into several ophthalmic prostaglandins and their derivatives. Using these strategy, we have obtained (±)-bimatoprost (1) and its analog, (±)-homobimatoprost (5). [ABSTRACT FROM AUTHOR]

Phthalic anhydride 1 was reacted with aromatic primary amines 2 in acetic acid at room temperature to yield mono acid mono amide derivatives 3. The latter were each transformed into the corresponding imides 4 by heating in the green solvent PEG-600 at 60°C high yields and in high purity in short reaction times involving a dehydrative ring closure. The above reaction of 1 with 2 in acetic acid was extended to succinic anhydride 5 and maleic anhydride 8 resulting in open chain compounds 6 and 9, respectively. The latter were cyclized, once again in the green solvent PEG-600, to the corresponding imides, i.e. succinimides 7 and maleimides 10, respectively. Each of the imides 4, 7, and 10 could be reconverted to the corresponding open chain compounds 3, 6, and 9 by heating in ethanolic KOH. Simple hydrolysis of imides 4, 7, and 10 with aq.H3PO4 yielded the corresponding dicarboxylic acids 11, 12, and 13, respectively. Treatment of maleic amide 9 and maleicimide 10 with Mg in EtOH under reflux gave the corresponding succinic amide 6 and succinicimide 7, respectively, by the chemo selective reduction of the double bond without touching the amide/carbonyl groups. [ABSTRACT FROM AUTHOR]

[image omitted] Knoevenagel condensation between indole-3-aldehyde 1 and an active methylene group containing 2,4-thiazolidinedione 2 in refluxing toluene using L-proline as a catalyst yielded 3, which on alkylation using 2 equivalents of alkylating agent under phase-transfer-catalyzed (PTC) conditions using K2CO3 as a base in dimethylformamide gave N,NI-symmetrically disubstituted 5-(1H-indol-3ylmethylene)-thiazolidine-2,4-diones 4. Alternately, 4 can be synthesized by condensing 5 and 6 in a single step. Using this synthetic strategy, N,NI-unsymmetricallydisubstituted derivatives 9a-f were prepared either by condensing 6 with N-substituted-2,4-thiazolidinedione 5 to obtain 7 followed by alkylation under PTC conditions or condensing 6 with N-unsubstituted- 2,4-thiazolidinedione 2 to yield 8 followed by alkylation under PTC conditions. The latter are the dehydro analogs of the dihydro-N-substituted-5-(1H-indol-3-yl-methylene)-thiazolidine-2,4-diones, which are potential antihyperglycemic agents. [ABSTRACT FROM AUTHOR]

Abstract: We report here a novel synthesis of 6-methyl-6H-7-oxopyrido[1,2-a]pyrimido[5,4-c]-1,2-benzothiazine-5,5-dioxide or cyclodehydration product of piroxicam, a metabolite detected in dogs and monkeys that was synthesized in 6% yield earlier. The reaction of benzoyl chloride with piroxicam in the presence of triethylamine afforded the piroxicam metabolite in good yield. A comparison of spectral data of the synthesized compound with the reported values remained inconclusive. The structure of the compound was confirmed unambiguously by single-crystal X-ray analysis. [Copyright &y& Elsevier]

Two unknown impurities in rofecoxib bulk drug at levels below 0.1% were detected by a simple isocratic reverse phase high performance liquid chromatography (HPLC). These impurities were isolated from crude sample of rofecoxib using reverse phase preparative HPLC. 1H, 13C and Mass spectroscopic investigations revealed the structures of the impurities as 4-[4-(methylsulphonyl)phenyl]-3-phenyl-5-hydroxyfuran-2-one (I) and 4-[4-(methylsulphonyl)phenyl]-3-phenyl-2,5-furandione (II), respectively. These structures were further confirmed by prepared synthetic standards of the impurities. The tentative mechanism for the formation of these impurities was discussed. [Copyright &y& Elsevier]

Bulk polar resistive humidity sensor with giant sensitivity (˜ 4600), large current hysteresis under small bias electric field, and many order of change in current/resistance in the range of relative humidity from 15% to 95% • A novel low cost polar resistive humidity sensor with a giant sensitive and long-term reproducibility. • The resistance of the sensor varies from GΩ to kΩ with a change in humidity from 15% to 95%. • An abrupt change in humidity sensing current with a change in polarity of bias voltage. • A digital display unit along with electronic circuitry developed to show the relative humidity. We report moisture sensitive properties of ferroelectric niobium-rich potassium tantalate K T a 0.2 N b 0.8 0.99 M n 0.01 O 3 (KTN) which shows giant humidity response with excellent reproducibility and repeatability of data as a function of exposure time and humidity contents. Many fold change in resistance was observed with change in the relative humidity (Rh) from 15% to 95% which provides maximum sensitivity (˜ 4600) at 298 K in the presence of Rh 95%. It also shows polarity dependent change in resistance with nearly 310 to 513 mV in-built potential depending on the device configuration. The polar KTN humidity sensor shows a decrease in resistance with an increase in Rh% which favors the Grotthuss mechanism responsible for humidity effects. To improve the sensitivity, a particular device configuration has implemented for the homogeneous interaction of the water vapor molecule with a maximum active sensor-surface area. The electronics with the digital display unit was designed and developed to represent the relative humidity in the form of digital display. [ABSTRACT FROM AUTHOR]

Three-component reaction involving condensation of 1-methyl quinoline-2,4(1 H,3 H)-dione 1, isatins 2(a-e), and malononitrile/cyanoacetic ester 3(a-b) in the task-specific ionic liquid [DBU][Ac] (1,8-diazabicyclo[5.4.0]-undec-7-en-8-ium acetate) leading to the spirooxindole derivatives 4(a-j) is described. This approach is affords the products in high yields without use of column chromatography and resulting compounds were evaluated for antibacterial activity against both gram positive and gram negative bacteria ( Staphylococcus aureus , Escherichia coli , Bacillus cereus, Bacillus subtilis, Salmonella typhimurium, and Klebsiella pneumonia). Among the all compounds, four compounds, that is, 4b, 4e, 4f, 4g, 4j exhibited moderate activity against all the strains as compared with the standard used. [ABSTRACT FROM AUTHOR]

A green and efficient synthesis of 4-heteryl-quinolines ( 9a, 9b, 9c, 9d), ( 10a, 10b, 10c, 10d) and ( 11a, 11b, 11c, 11d) has been described using PEG-600 as a green solvent. Initially, 4-chloro-2-methylquinolines ( 5a, 5b, 5c, 5d) on reaction with aromatic heterocyclic thiols ( 6), ( 7), and ( 8) using PEG-600 at 100°C for 30-40 min resulted in ( 9), ( 10), and ( 11) in good yields. Alternatively, ( 9), ( 10), and ( 11) could also be prepared in dimethylformamide using K2CO3 as base and tetrabutylammonium bromide as phase transfer catalyst at 100°C for 1-2 h. All the compounds were synthesized and characterized by IR, NMR, mass spectroscopy, and 13C NMR analysis. All synthesized compounds were screened for their against clinical strains that include Gram-positive (Bacillus subtilis MTCC 121, staphylococcus aureus MLS-16 MTCC 2940, Micrococcus lutes MTCC 2470, and Staphylococcus aureus MTCC 96) and Gram-negative bacteria (Candida albicans MTCC 3017, Klebsiella planticola MTCC 530, Escherichia coli MTCC 739, and Pseudomonas aeruginosa MTCC 2453). The results revealed that compounds ( 9a, 9d, 10a, 10c, 11b, and 11d) exhibited significant almost equal to the standard drug, that is, Ciprofloxacin. [ABSTRACT FROM AUTHOR]

Green synthesis of novel title compounds (6) has been developed from 3-(1,4-dioxo-3,4-dihydrophthalazin-(1H)-yl)-3-oxopropanenitrile (3) and indole-3-aldehyde (4) using Knoevenagel condensation followed by alkylation with alkylating agents. Compound 6 could also be synthesised by alkylation of 4 followed by condensation with 3. In an alternate sequence of reactions, 6 could be synthesised either from treatment of 3 with N,N-dimethylformamide dimethyl acetal to form (E)-3-(dimethlamino)-2-(1,4-dioxo-1,2,3,4-tetrahydrophthalazine-2-carbonyl)acrylonitrile 8 followed by reaction with 10 or by the reaction 8 with 9 followed by alkylation. [ABSTRACT FROM AUTHOR]

Facile, efficient, four-component domino reaction of dialkylphthalates, hydrazine hydrate, indole-3-carboxaldehydes, and malononitrile/ethyl cyanoacetate leads to the formation of 1-(1H-indol-2-yl)-1H-pyrazolo [1,2-b] phthalazine-5,10-diones in the presence of InCl3as catalyst in refluxing ethanol for 1 h in good yields. This four-component domino reaction transformation presumably proceeds via sequential addition, dehydration, condensation, and cyclization steps. [ABSTRACT FROM PUBLISHER]

The asymmetric synthesis of both the enantiomer of chiral amines from the single chiral source of N-tert-butylsulfinylaldimines (3) by simply changing the organometallic reagents through diastereoselective addition. An efficient enantioselective synthesis of chiral amines including (S)-3-methyl-1-(2-piperidin-1-yl-phenyl)butyl amine (6a), a key intermediate to prepare antidiabetic drug repaglinide (1), is reported. [ABSTRACT FROM PUBLISHER]

A series of indolylidinepyrazolones were synthesized using a simple, green, and effective route and evaluated as anti-bacterial agents. The compounds were further studied via structure-guided docking study. One of the compounds exhibiting H-bonding interactions with conserved residue Arg144 turned out to be the most potent compound of the series. The minimum inhibitory concentration values ranged from 50 to 25 μg/mL against Staphylococcus aureus in their anti microbial evaluation. [ABSTRACT FROM AUTHOR]

Indium chloride has been used as a versatile Lewis acid catalyst for the synthesis of 3-sulfenylindoles in good yields by the independent reaction of indoles and N-alkylindoles withN-(phenylthio)phthalimide in dimethyl formamide (DMF) at 100°C for about 5–6 h. [ABSTRACT FROM AUTHOR]

Abstract: Green and efficient one pot, three-component synthesis of novel 2-amino-6-(1,4-dioxo-3,4-dihydrophthalazin)-2(1H)-yl-4-phenyl-4H-pyran-3,5-dicarbonitriles 6 has been developed by condensing 3-(1,4-dioxo-3,4-dihydrophthalazin-(1H)-yl)-3-oxopropanenitrile 3, benzaldehydes 4 and active methylene compounds 5 using l-proline as catalyst in EtOH at RT. [Copyright &y& Elsevier]

S-(+)-Clopidogrel bisulfate [(S-(+)-methyl 2-(2-chlorophenyl)-2-(6, 7-dihydrothieno[3, 2-c]pyridin-5(4H)-yl)acetate bisulfate)] is a platelet aggregation inhibitor drug. S-(+)-Clopidogrel bisulfate is prepared by different synthetic approaches in the literature. In almost all the approaches the major impurities known in the literature (A, B, and C) are also listed in the U.S. pharmacopoeia. The control of these pharmaceutical impurities is currently a critical issue to the pharmaceutical industry. In this article, a description of these impurities and their origins in the S-(+)-clopidogrel bisulfate process are presented along with the preparation of impurity B. [ABSTRACT FROM PUBLISHER]

Abstract: The design, synthesis and SAR of novel tetrahydrocarbazole derivatives having 5-HT6 receptor antagonist activity is presented. The racemic compound 15e was found to possess desirable pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition. [Copyright &y& Elsevier]

Abstract: A number of novel 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles based on a conformationally restricted pyrazole framework have been designed as potential inhibitors of PDE4. All these compounds were readily prepared by using simple chemistry strategy. The in vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized along with the X-ray single crystal data of a representative compound is presented. [Copyright &y& Elsevier]

Abstract: A series of novel 6-fluoro1,4-dihydro-4-oxo-3-quinoline carboxylic acid dimers were synthesized as potential antibacterial agents from commercially available substituted fluorobenzoic acids. A stability indicating HPLC method was developed to determine these novel fluoroquinolone dimers using a systematic method development approach. Samples were subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation; and analyzed to demonstrate the specificity and stability indicating ability of the developed method. The precision for all four fluoroquinolone dimers was within 2.0% RSD. Calibration curves were linear (LOQ, 150%), with regression coefficients >0.99 for all dimers. The method was conveniently applied for determining purity and assay of these four novel fluoroquinolone dimers. [Copyright &y& Elsevier]

Abstract: A simple and rapid capillary zone electrophoretic method was developed for determining dimethyl sulfate a possible human carcinogen and mutagen and chloroacetyl chloride a potential genotoxic agent at trace levels in pharmaceutical drug substances by indirect photometric detection. A systematic screening of various anionic probes was performed to obtain the best separation conditions and sensitivity. High sensitivities with low quantification and detection levels were achieved for dimethylsulfate and chloroacetyl chloride using a background electrolyte (BGE) containing 5mM pyridine dicarboxylic acid as the probe ion. The method is specific, precise and accurate for the two genotoxins. The optimized method was validated for specificity, precision, linearity, accuracy and stability in solution. Calibration curves were linear (R >0.999) for both dimethylsulfate and chloroacetyl chloride in the range LOQ – 300% of nominal concentrations. The CE method was effectively implemented for estimating dimethylsulfate and chloroacetyl chloride in two different active pharmaceutical ingredients (APIs). [Copyright &y& Elsevier]

Several functionalized thienopyrimidines were synthesized by a facile synthetic method, which includes Gewald's reaction, and were characterized by spectral and analytical data. These functionalized thienopyrimidines were converted to various new chemical entities of biological importance, such as 2-piperazinymethyl thienopyrimidines (6, 8), 4-dimethylaminoethoxy thienopyrimidines (11), and 3-dimethylaminoethyl thienopyrimidines (12). All the compounds thus synthesized were screened for their invitro biological activities. Some of the compounds displayed promising serotonin 5-HT6 receptor antagonist activities. [image omitted] [ABSTRACT FROM AUTHOR]

Abstract: A series of N 1-arylsulfonyl-3-(pyrrolidin-3-yl)-1H-indole and N 1-arylsulfonyl-3-(4-chloro-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole derivatives (tryptamine derivatives with rigidized side chain) have been prepared and tested for their binding affinity to 5-HT6 receptor. Several compounds displayed potent binding affinity for the 5-HT6 receptor when tested in in vitro binding assay. The primary SAR indicates that rigidification of dimethylamino alkyl chain at C3 of indole carbon maintains the binding affinity to 5-HT6R. The lead compound N 1-benzenesulfonyl-3-(4-chloro-1-methyl-2,5-dihydro-1H-pyrrol-3-yl)-1H-indole, 10a (K b =0.1nM) has shown excellent in vitro affinity and was active in animal models of cognition like NORT and water maze. [Copyright &y& Elsevier]

A tropospheric ozone variability study is carried out to investigate the spatial and temporal distribution over the coastline of the Indian peninsula and adjacent land and sea using NASA Langley Tropospheric Ozone Residual data set for the period 1979-2005. A strong seasonal cycle has been observed with large variation (∼ 55%) over the upper eastern coast, followed by the upper and lower western coast, compared to the lower eastern coast (∼ 33%). A negative gradient in ozone concentration is observed along eastern and western coasts during summer (slope ∼ -0.78 and -0.65) and a positive gradient (slope ∼ 0.16 and 0.21) during winter. The same is observed over the adjacent land and sea along the coastline with slight variation. This change in gradient can be attributed to the anthropogenic emission of precursor gases that reinforce localized photochemical production of ozone. In addition, topography, transport, seasonality of emission of precursor gases and the solar insolation cycle play a vital role. [ABSTRACT FROM AUTHOR]

Abstract: N 1-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT6 receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT6 receptor. The compound 7a (K i =3.4nM, functional assay IC50 =310nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter. [Copyright &y& Elsevier]

Abstract: A series of novel aryl aminosulfonamides was designed and synthesized as 5-HT6 receptor ligands. Many compounds screened in a functional reporter gene based assay displayed potent antagonistic activity with Kb values in the range of 0.02–10nM. The lead compound 11m exemplified in this series showed good ADME surrogate properties, acceptable pharmacokinetic profile and is active in animal models of cognition like novel object recognition test and Morris water maze. The compound was selected for detailed profiling. [Copyright &y& Elsevier]

To study tropospheric ozone variability over the Indo-Gangetic (IG) basin, monthly tropospheric ozone residual (TOR) data has been analysed for the 1979-2004 period. Tropospheric column ozone has been observed to have a maximum during late summer (48 ± 4.1 DU) and a minimum during late winter (30 ± 4.2 DU) over the IG basin. The amplitude of the seasonal cycle has been observed to be comparatively larger over the western part of the IG region (∼51 ± 2.3 DU) than over the central (∼47 ± 3.2 DU) and eastern parts (∼47 ± 3.2 DU) of the region. Similarly, the seasonal variation in tropospheric ozone has been observed to be comparatively larger over the western part of the IG region (∼22 DU) than over the central (∼18 DU) and eastern parts (∼17 DU) of the region. The difference in tropospheric ozone amount over the eastern and western parts of the IG region also shows seasonal variation with a large difference (up to 4 DU) during the monsoon season. The monsoon system plays an important role in the seasonal variation of the tropospheric ozone over the different parts of the IG region. [ABSTRACT FROM AUTHOR]

Abstract: A highly sensitive and enantioselective assay has been developed and validated for the estimation of torcetrapib (TTB) enantiomers [(+)-TTB and (−)-TTB] in hamster plasma with chiral liquid chromatography coupled to tandem mass spectrometry with an atmospheric pressure chemical ionization interface in the negative-ion mode. The assay procedure involves liquid–liquid extraction of TTB enantiomers and IS (DRL-16126) from 100μL hamster plasma with acetonitrile. TTB enantiomers were separated using n-hexane:propanol (80:20, v/v) at a flow rate of 0.7mL/min on a Chiralpak AD column. The MS/MS ion transitions monitored were 599.2→340.2 for TTB and 623.2→298.1 for IS. Absolute recovery was found to be between 64 and 68% for TTB enantiomers and >100% for IS. The standard curves for TTB enantiomers were linear (r 2 >0.995) in the concentration range 5–2500ng/mL for each enantiomer with an LLOQ of 5ng/mL for each enantiomer. The inter- and intra-day precisions were in the range of 10.5–12.4 and 9.15–11.5% and 3.75–12.9 and 5.16–12.5% for (+)-TTB and (−)-TTB, respectively. Accuracy in the measurement of quality control (QC) samples was in the range 91.3–105 and 88.6–111% for (+)-TTB and (−)-TTB, respectively. This novel method has been applied to the study of stereoselective oral pharmacokinetics of (−)-TTB. [Copyright &y& Elsevier]

Negatively charged magnetic liposomes were prepared using soya lecithin (Soya PC), cholesterol and phosphatidyl serine (PS) for their preferential presentation to circulating blood phagocytes (monocytes and neutrophils). PS ratio was optimized in terms of drug and magnetite loading, in vitro magnetic responsiveness and ex vivo monocytes/neutrophils uptake. RGD peptide was covalently coupled to the negatively charged liposomes composed of PC, cholesterol, PS and phopsphatidyl ethanolamine (PE) via carbodiimide-mediated coupling. In vivo cellular sorting study under magnetic guard indicated an increase in relative count of neutrophils and monocytes. Results suggest that selective uptake of RGD-anchored magnetic liposomes by these cells imparts them magnetic property. High levels of a model drug diclofenac sodium was quantified in target organ brain. In case of negatively charged uncoated magnetic liposomes brain levels of the drug was 5.95-fold compared to free drug and 7.58-fold in comparison to non-magnetic formulation, while for RGD-coated magnetic liposomes this ratio was 9.1-fold compared to free drug solution, 6.62-fold compared to non-magnetic RGD-coated liposomes and 1.5-fold when compared to uncoated magnetic liposomes. Liver uptake was significantly bypassed (37.2% and 48.3% for uncoated and RGD-coated magnetic liposomes, respectively). This study suggested the potential of negatively charged and RGD-coated magnetic liposomes for monocytes/neutrophils-mediated active delivery of drugs to relatively inaccessible inflammatory sites, i.e. brain. The study opens a new perspective of active delivery of drugs for a possible treatment of cerebrovascular diseases. [Copyright &y& Elsevier]

Three unknown impurities and a byproduct in repaglinide bulk drug at levels below 0.1% (ranging from 0.05 to 0.1%) were detected by a simple isocratic reversed-phase high performance liquid chromatography (HPLC) method. These impurities were isolated from crude sample of repaglinide using reversed-phase preparative high performance liquid chromatography. Based on the spectroscopic data (IR, NMR and MS) the structures of these impurities (I, II and IV) and byproduct (III) were characterised as 4-carboxymethyl-2-ethoxy-benzoic acid (I), 4-cyclohexylaminocarbamoylmethyl-2-ethoxy-benzoic acid (II), 1-cyclohexyl-3-[3-methyl-1-(2-piperidin-1-yl-phenyl)-butyl]-urea (IV) and 1,3-dicyclohexyl urea (III), respectively. Their synthesis and formation is discussed. [Copyright &y& Elsevier]