Search

A series of halogenated chalcones (3–8) was synthesized and confirmed by several spectral tools. The cytotoxic effect of this series was tested against a panel of different cancer cell lines (MCF7, A549, HCT116, and PC3). Our MTT assay results revealed that chalcone 8 had the potent cytotoxic activity against all tested cancer cell lines except A549 cells, which were more sensitive to chalcone 7 relative to the positive control treated with doxorubicin. Chalcone 8 showed the least cytotoxic activity against the normal epithelial cell line RPE-1 and the lowest IC50 at 10.96 µM relative to the IC50 of the chemotherapeutic drug doxorubicin at 12.8 µM against the human breast cancer cell line MCF7. Molecular docking studies showed a good interaction of chalcone 8 with the active site of histone demethylase (PLU-1/ JARID1B) and Carboxy-terminal binding protein1 (CtBP1) proteins. Mechanistically, chalcone 8 induced cell cycle arrest at G2/M phase and apoptosis as assessed by flow cytometry, as well as DNA fragmentation in MCF7 cells. Chalcone 8 upregulated mRNA expression levels of the apoptotic genes BAX, p53, and Caspase-7, Caspase-8, and Caspase-9, whereas mRNA expression levels of the antiapoptotic gene Bcl2, metastasis-related gene matrix metalloproteinase 1, and the autophagic markers ATG5 and LC3B were downregulated as quantified by qPCR.

Respiratory infection is one of the infections that can be transmitted in closed places due to the ease of transmission of pathogens from infected people to healthy people through droplets from coughing and sneezing, among these bacterial causes, Haemophilus influenza. Therefore, this study aimed to evaluate the prevalence of this type of bacteria among pilgrims coming from different geographical locations in the world and determine the antibiotic-resistant strains. Around 1226 nasopharyngeal swabs were collected from 613 pilgrims from several different nationalities before and after completing the Hajj. These specimens were cultivated on chocolate agar medium and the pathogens were identified according to Clinical Laboratory Standards Institute (CLSI) protocol and confirmed by an automated system machine (VITEK2). There is no H. influenzae was detected among pilgrims before performing Hajj and the rate of transmission of H. influenzae was 1% after performing Hajj. The most effective antibiotics against to H. influenza isolates from pilgrims was Rifampicin while all the isolates were resistant to ampicillin. The continuous monitorization of the rate of potentially pathogenic bacterial during the Hajj season is required in order to develop advanced strategies to confront any outbreak of any infectious disease among the pilgrims. Key words: Hajj season, nasopharyngeal swabs, ethnic group, Makkah.

The emergence and spread of multidrug-resistant microorganisms are threats to public health due to its related increasing rates of morbidity and mortality in the world. Routine disinfection practices do not eliminate many of these resistant species and may contribute to the development in their resistance. Therefore, the current study evaluates the effectiveness of some popular detergents labelled as antibacterial and available at local market. Fifteen different brands of detergents were tested against thirteen American-type culture collection (ATCC) strains; five species related to Gram-positive bacteria, eight species to Gram-negative bacteria and three clinical isolates, (Escherichia coli, Klebsiella pneumonia and Methicillin resistant Staphylococcus aureus (MRSA) by measuring their efficacy by agar well diffusion technique and contact time assay. Dilution levels of detergents exhibited different zones of inhibition against the tested bacterial strains. The initial dilutions of detergents (DAC, SUNOVA, CLOROX, Drummer, GENTO, Dettol with pine, Dettol, Clorox Original, EMLAG and 3 M) showed inhibition zones ranging from 10 mm to >40 mm on Gram positive bacteria. Dettol, Clorox Original, EMLAG and 3 M showed inhibition zones ranging from 11 to 20 mm on limited numbers of Gram-negative bacteria at the first dilutions of detergents. The results showed that, Dettol, Clorox and 3 M were the strongest detergents compared to the other detergents included in this study. A contact-time assay showed a positive relationship between exposure time and efficacy of detergent against the tested bacterial strains. Key words: Detergents, multidrug-resistant microorganisms, nosocomial infection, Makkah.

Two novel chemotherapeutic chalcones were synthesized and their structures were confirmed by different spectral tools. Theoretical studies such as molecular modeling were done to detect the mechanism of action of these compounds. In vitro cytotoxicity showed a strong effect against all tested cell lines (MCF7, A459, HepG2, and HCT116), and low toxic effect against normal human melanocytes (HFB4). The lung carcinoma cell line was chosen for further molecular studies. Real-time PCR demonstrated that the two compounds upregulated gene expression of (BAX, p53, casp-3, casp-8, casp-9) genes and decreased the expression of anti-apoptotic genes bcl2, CDK4, and MMP1. Flow-cytometry indicated that cell cycle arrest of A459 was induced at the G2/M phase and the apoptotic percentage increased significantly compared to the control sample. Cytochrome c oxidase and VEGF enzyme activity were detected by ELISA assay. SEM tool was used to follow the morphological changes that occurred on the cell surface, cell granulation, and average roughness of the cell surface. The change in the number and morphology of mitochondria, cell shrinkage, increase in the number of cytoplasmic organelles, membrane blebbing, chromatin condensation, and apoptotic bodies were observed using TEM. The obtained data suggested that new chalcones exerted their pathways on lung carcinoma through induction of two pathways of apoptosis. Graphical abstract Novel chalcones were prepared and confirmed by different spectral tools. Docking simulations were done to detect the mechanism of action. In vitro cytotoxicity indicated a strong effect against different cancer cell lines and low toxic effects against normal human melanocytes (HFB4). The lung carcinoma cell line was chosen for further molecular studies that include Real-time PCR, Flow-cytometry, Cytochrome c oxidase, and ELISA assay. SEM and TEM tool were used to follow the morphological changes occurred on the cell surface.

Objective: Coupling of ethyl 2-(6,7-dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate 2 with diazotized anilines in ethanol in the presence of sodium acetate yielded 2-(2-arylhydrazono)-2-(6,7- dimethoxy-3,4-dihydroisoquinolin-1-yl)acetate (4a-f). Methods: Treatment of 2 with α-bromoketones 6a-f in dry benzene at reflux gave the corresponding isoquinolinium bromides 7a-f. Refluxing of each of the salts 7a-f in dry benzene and in the presence of triethylamine yielded 2-arylpyrrolo-[2,1-a]isoquinoline structures 8a-f, that converted to ethyl (E)-8,9- dimethoxy-3-(phenyldiazen-yl)-2-(aryl)-5,6-dihydropyrrolo[2,1-a]isoquinoline-1-carboxylate (9a-f) upon treatment with diazotized anilines 3 in ethanol in the presence of sodium acetate. Results and Conclusion: Cytotoxic assay was performed for in vitro antitumor screening against caucasian breast adenocarcinoma (MCF7), hepatocellular carcinoma (HepG2) and colorectal carcinoma (HCT-116) cell lines. The results were compared with the standard anticancer drug (doxorubicin). Molecular docking using MOE 2014.09 software was carried out for the most potent compound 4d, which showed the highest binding affinity towards the four tested proteins and thus initiated apoptosis of cancer cells.

Schiff bases exhibited various pharmacological and biological activities such as antibacterial, cytotoxic effects, antifungal, and antimalarial. Schiff bases were used for designing organic compounds, metal complexes, or nanoparticles. Also, Schiff bases were applied in various fields as corrosion inhibitors, catalysts, and optical properties. Therefore, this review article focused on some synthesis, reactions, applications, and biological activities of Schiff bases especially Schiff bases-heterocyclic moiety conjugates in the ten last years.

Electrocardiography is the principle of recording the electrical activity of the heart over finite duration of time. It is one of the most practiced methods to detect abnormalities in the heart's electrical, arterial and muscular systems. Electrocardiogram is the voltage versus time graph obtained from the Electrocardiography machine. Automated analysis makes detection of Electrocardiogram findings and consequently determination of pathological abnormalities without human intervention possible. To achieve this goal we process digital Electrocardiograms to quantify the amplitudes and durations of waves and intervals, that is necessary for the automated analysis to find the pathological abnormalities. The proposed method processes Electrocardiograms and localizes the P, Q, R, S and T waves, subsequently it measures the PR, QT and ST intervals and segments.

Electrocardiography is the principle of recording the heart muscle’s action potentials. It is a primary method in detecting the electrical abnormality of the heart. The graph generated by an electrocardiograph shows the temporal characteristics of the voltage across the heart and different body locations. The graph is composed of many parts designated as waves (P, Q, R and S waves), segments (QT segment) and intervals (PR and RR intervals). Detecting these components is important to extract the features of the electrocardiogram and consequently determine whether the electrocardiogram is normal or abnormal. The first component to be detected in the electrocardiogram is the R wave because of its distinct morphology of sharp deflections. This paper proposes a method to localize the R waves by setting a static threshold value that its magnitude depends on the electrocardiogram's statistical properties. The threshold value is unique to every rhythm, and it is determined by calculating the population of each quantization level and subsequently finding the most repeated population figure and the quantization level associated with it. This level stands as the threshold to detect the R waves.

Electrocardiography is a medical test in the diagnosis of various cardiac abnormalities. Signal processing techniques are used to analyze Electrocardiograms digitally. This paper proposes a method to detect the R waves in the Electrocardiogram rhythms with no threshold being set in priori (neither static nor time-varying). The proposed method modulates the Electrocardiogram by implementing linear amplitude amplification, then detects the peaks in the Electrocardiogram according to the mathematical definition of a peak with an additional criterion that the peak must be greater than all preceding peaks. The Electrocardiogram amplitude corresponding to the maximum derivative magnitude of the descending amplitude sequence of the peaks is set to be the threshold which differentiates between unwanted peak detections made in the primary stage and the desired peaks.

Depending on the reaction conditions, two alternative cyclizations are possible for [3 + 3] cyclocondensation of pyrazolone derivative 1a and ethyl cyanoacetate of type pyrano [2,3-c] pyrazol-6(1H)-one 2 and pyrano [2,3-c] pyrazol-4(1H)-one 3. Keeping of enaminic system 3 and benzylidene malononitrile in the presence of catalytic amount of trimethylamine resulted in pyridine cyclization affording pyrazolopyranopyridine derivative 4, not 5. The pyrazolone derivative 6a was obtained as a result of the acid-mediated addition reaction between compound 1a, urea and/or ammonium thiocyanate. In addition, the bispyrazolone of type 6b was obtained from the condensation reaction of urea and pyrazolone derivative. The spiro compound 7 was obtained from the double-addition reaction of pyrazolone to cinnamoyl isothiocyanate. A one-pot three-component condensation of a 3-hydroxybenzaldehyde, pyrazolone 1a, urea and/or thiourea under Biginelli conditions resulted in tetrahydropyrazolo pyrimidine derivatives 8a and 8b, respectively. The acid-mediated reaction of benzaldehyde and pyrazolone derivative 1a in the presence of Ac2O yielded styrylpyrazole derivative 9. The polyfunctionalized product 9 reacted with hydrazine to furnish pyrazolotriazoloe of type 10. Treatment of styrylpyrazole derivative 9 with aniline furnished the aniline derivative 11 and none of the expected polyheterocyclic derivative 12 was obtained. Compound 9 undergoes pyridine cyclization to produce 13 under the effect of urea. N-phenyl pyrazolone converted into pyrano-dipyrazolone derivative 14. Pyran of type 14 underwent a ring transformation upon treatment with urea and/or thiourea to give the same dipyrazolo pyrimidine derivative 15. The newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, ESI/LC-MS and elemental analysis.

Traditional yoghurt (TY) (Streptococcus thermophiles+ Lactobacillus bulgaricus) and Bifidus yoghurt (BY) samples(Streptococcus thermophiles+ Lactobacillus bulgaricus+ Bifidobacterium bifidum). Traditional & Bifidus yoghurtsamples were inoculated with 106 cfu/g L. monocytogenes and stored for 21 days at 4±1oC. Samples were taken at zerotime (fresh samples) then after 3, 5, 7, 10, 14 and 21 days of storage for titratable acidity measurement and bacterial countof the culture starters and L. monocytogenes counts. The results revealed that the titratable acidity of TY & BY wasincreased during the 21 days of storage, while the population of L. monocytogenes became non-detectable level in 10thdays of storage in BY and still detected in TY till the day 14th of storage and became 2.20± 0.31 log10 cfu/g. The countof all starter cultures (S. thermophiles+ Lb. bulgaricus+ B. bifidum) in both yoghurts increased during the fermentationand cold storage and remained stable with values >6 log10 cfu/g throughout the storage period at 4±1°C.

The survival of Staphylococcus aureus in the acidophilus yoghurt (AY) was evaluated during the production and coldstorage. 21 acidophilus yoghurt samples were prepared with traditional yoghurt culture (Streptococcus thermophiles &Lactobacillus bulgaricus) with Lactobacillus acidophilus and inoculated with 106 cfu/ml S. aureus and stored for 21 daysat 4oC. Samples were taken at zero time (fresh samples), 3, 5, 7, 10, 14 and 21 days for titratable acidity, culture starters’counts and S. aureus count. The results revealed that the titratable acidity% of AY was increased and reached 0.72, 0.78,0.83, 0.87, 0.89, 1.02 and 1.45% at zero time, 3, 5, 7, 10, 14, and 21 days of storage, respectively, while the population of S. aureus reached 6.10 and 3.70 log10cfu/g at zero time and 3rd day of storage, respectively and became non-detectable level in 5th days of storage. The count of all starter cultures (S. thermophiles+ L. bulgaricus+ L. acidophilus) in acidophilus yoghurt increased during the fermentation and cold storage, S. thermophiles became 7.15, 7.35, 8.20, 8.15, 7.45, 7.45 and 6.65 log10cfu/g while L. bulgaricus 7.25, 7.55, 8.25, 8.73, 7.76, 7.47 and 6.54 log10cfu/g and L. acidophilus became 7.38, 7.70, 8.25, 8.20, 7.50, 7,46 and 6.66 log10cfu/g at zero time, 3, 5, 7, 10, 14, and 21 days of storage, respectively. It concluded that S. aureus count decreased gradually during the production and cold storage and became non-detectable level on the 5th days of cold storage. The survival of all starter cultures in yoghurt sample remained stable with values > 6 log10 cfu/g throughout the storage period at 4±1°C.

Objective: To detect the prevalence of carbapenem resistance among Gram negative bacilli at the Al-Noor Specialist Hospital in the western part of Saudi Arabia. Materials and Methods: This study was conducted in the Microbiology department, Al-Noor Specialist Hospital, Makah city, Saudi Arabia. The clinical samples were collected from admitted patients in the wards, Intensive Care Units (ICUs), urology unit and surgery unit, these samples included blood, urine, sputum, pus and wound. The identification and antibiotic susceptibility testing of all bacterial isolates were performed via the Vitek 2 Compact System. Results: Out of 4803 Gram negative bacterial bacilli were isolated, the prevalence rate of carbapenem resistance among these isolates was 2797/4803 (58.23%), and sensitivity rate was 2006/4803 (41.77%) of the total isolates. The rate of resistance to carbapenem was among Acinetobacter baumannii 1710 (99.13%), followed by Pseudomonas aeruginosa 575 (62.4%), Klebsiella pneumoniae 459 (38%) and Escherichia coli 56 (5.59%). The trend of carbapenem resistance among Gram negative bacterial isolates from 2013-2015 was 53.99%, 59.88% and 61.43% respectively. Conclusion: A. baumannii rec-orded, the highest rate of carbapenem resistance through three year, 98.19%, 99.48% and 99.81% respectively and the lowest rate of resistance recorded with E. coli, 4.63%, 5.79% and 6.31% respectively.

Highly pathogenic avian influenza (HPAI) H5N1 virus continues to undergo substantial evolution. Emergence of antiviral resistance among H5N1 avian influenza viruses is a major challenge in the control of pandemic influenza. Numerous studies have focused on the genetic and evolutionary dynamics of the hemagglutinin and neuraminidase genes; however, studies on the susceptibility of HPAI H5N1 viruses to amantadine and genetic diversity of the matrix (M) gene are limited. Accordingly, we studied the amantadine susceptibility of the HPAI H5N1 viruses isolated in Egypt during 2006–2015 based on genotypic and phenotypic characteristics. We analyzed data on 253 virus sequences and constructed a phylogenetic tree to calculate selective pressures on sites in the M2 gene associated with amantadine-resistance among different clades. Selection pressure was identified in the transmembrane domain of M2 gene at positions 27 and 31. Amantadine-resistant variants emerged in 2007 but were not circulating between 2012 and 2014. By 2015, amantadine-resistant HPAI H5N1 viruses re-emerged. This may be associated with the uncontrolled prescription of amantadine for prophylaxis and control of avian influenza infections in the poultry farm sector in Egypt. More epidemiological research is required to verify this observation.

Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites that are reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity. In addition, heterocyclic compounds having nitrogen such as isoquinolines are of considerable interest as they constitute the core structural element of many alkaloids that have enormous pharmacological activities. Objective: The objective of this study is the synthesis and biological activity of novel chalcones incorporating thiadiazolyl isoquinoline as potential anticancer candidates. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Methods: An efficient one pot synthesis of novel chalcones incorporating thiadiazolyl isoquinoline has been developed. The cytotoxic activity of the novel synthesized compounds was performed against four different kinds of cancer cell lines. Results: Among all the tested derivatives, chalcone 3 has the best cytotoxic profile against A549, MCF7, and HeLa cell lines, with IC50s (66.1, 51.3, and 85.1μM, respectively). Molecular docking studies for chalcone 3 revealed that CDK2, and EGFRTK domains have strong binding affinities toward the novel chalcone 3, while tubulin-colchicine-ustiloxin, and VEGFRTK domains illustrated moderate mode of binding. Conclusion: We have developed an efficient method for the synthesis of novel chalcones incorporating thiadiazolyl isoquinoline. All compounds showed better cytotoxicity results against four kinds of cancer cell lines (A549, MCF7, HCT116, and HELA cells). The results depicted that chalcone 3 has a high and promising cytotoxic effect against HELA cell line and the mechanism of cytotoxicity was widely studied through different theoretical and experimental tools. Thus, the newly synthesized derivative 3 can be utilized as a novel chemotherapeutic compound for cervical carcinoma.

Background Elevated N-terminal of the prohormone brain natriuretic peptide (NT-proBNP) concentrations in childhood epilepsy and febrile convulsions has been reported. The present study was conducted on 30 children at Alexandria University Children's Hospital. They have been classified into two groups: (1) seizures group which included 20 postictal children (10 males and 10 females), subdivided into 10 children with partial epilepsy who had partial motor seizures (PS) and 10 children with idiopathic generalized epilepsy who had tonic–clonic seizures and (2) control group which included 10 children (8 males and 2 females) who was randomly selected from epileptic children after a seizure-free period of at least for 2 months. All cases and controls were subjected to full history taking, clinical examination with emphasis on neurological examination, and routine laboratory investigations to exclude any disease that may alter serum level of BNP, such as cardiac, renal, or hepatic disease. For seizures group, plasma concentration (NT-proBNP) was measured within 4 hours after seizure onset and again 24 to 48 hours later. For control group NT-proBNP was measured once. Subanalyses were done and plasma NT-proBNP levels in each subgroup of postseizure group within 4 hours postictal were compared with NT-proBNP levels among control group. Results NT-proBNP plasma concentrations within 4 hours postictal were significantly higher among the postseizure group compared with the control group. Significant decrease of NT-proBNP levels in the postseizure group was observed after the 24- to 48-hour follow-up. NT-proBNP plasma concentrations were significantly higher among patients with generalized seizures compared with controls. Conclusion Plasma NT-proBNP assay when measured in the appropriate clinical setting may be useful in the diagnosis of childhood epilepsy.

Two series of metronidazole derivatives (ester derivatives and ether derivatives) were prepared reacting metronidazole and its acetic acid oxidized form with menthol, thymol, carvacrol, and eugenol. Both series of compounds were tested in vitro against two strains of Helicobacter pylori (the ATCC 26695 and P12), and one strain of Clostridium (Clostridium perfringens). Most of the prepared compounds showed biological activity against the targeted bacteria. Compound 11 was highly active against all tested bacterial strains, especially against P12 with IC50 0.0011 μM/ml. Compound 6 was highly active against C. perfringens with MIC 0.0094 nM/ml. Viability test was conducted for compound 11 to test its selectivity for normal human fetal lung fibroblasts (MRC5), and it was found to be non-toxic with IC50 more than 50 μM/ml.

The aim of this study was to the evaluation of frequency and distribution of Serratia marcescens in the hospital departments and determination of antimicrobial resistance of the isolated strains. Methods: The study included 81 Serratia marcescens strains isolated from 61 patients hospitalized in the in the different hospital wards of Al-Noor Specialist Hospital within the period from 1/11/2012 to 1/11/2013. The strains were isolated from wound swabs, blood cultures, sputum, urine culture, fluid, catheter and throat swab, wound swabs, blood cultures and cerebrospinal fluid. Results: The isolates were identified by conventional method and the results and susceptibility testing were confirmed by VITEC-2 Compact. Most frequently Serratia marcescens has been implicated in ICU [21%] followed by male medical [18.5%] and emergency department [12.3%]. The resistance of Serratia strains was high, excepting imipenem (15%), Meropenem (27) and the resistance was higher with ampicillin (97.5%), Cefoxitin (90%) and Tetracycline (86%). Conclusion: Continuous monitoring of nosocomial infections is indispensable. Phenotypic characterization of the isolates is useful for studying the relationship of microbial pathogens.

More than half of the patients undergoing laparoscopic cholecystectomy experience postoperative nausea and vomiting (PONV). This condition is related to the surgical, anesthetic, and patient factors. Volatile anesthetics, nitrous oxide, and opioids are known anesthetic risk factors for PONV, and thus preventive measures are justified. Propofol-based total intravenous anesthesia (TIVA), ondansetron, and dexamethasone each are reported to reduce PONV by approximately 30%. Avoiding or reducing perioperative narcotic analgesics, use of an 80% oxygen concentration, and proper intravenous fluid administration also reduce PONV. The anesthetic antiemetic measures have been studied separately. This study aimed to test the efficacy of these anesthetic antiemetic measures collectively with or without ondansetron or dexamethasone in preventing PONV among patients undergoing laparoscopic cholecystectomy. For this study, 160 patients undergoing laparoscopic cholycestectomy (33 males and 147 females) were randomized into one of three groups. Group O received 4 mg of ondansetron; group D received 8 mg of dexamethasone; and group P received normal saline immediately after induction of anesthesia. All the patients received propofol-based TIVA, 80% oxygen concentration, 20 ml/kg of Hartman’s solution, and 1.5 mg/kg of tramadol. Opioids, nitrous oxide, and volatile anesthetics were not used for any patient. Episodes of PONV were recorded at 0- to 4-h and 4- to 24-h intervals. The incidences of PONV were 32% in the ondansetron group, 30% in the dexamethasone group, and 33% in the saline group. There were no significant differences among the groups (p > 0.05). Ondansetron or dexamethasone added to collective anesthetic antiemetic measures does not further decrease the incidence of PONV after laparoscopic cholycestectomy.

Problem statement: The purpose of this study was to evaluate the onset and duration of sensory and motor block as well as operative analgesia and adverse effects of Dex Metedo Midine (DXM) or fentanyl given intrathecally with plain 0.5% bupivacaine for spinal anesthesia. Approach: seventy six patients classified as American Society of Anesthesiologists (ASA) status I, II and III scheduled for vaginal hysterectomy, vaginal wall repair and tension free vaginal tape were prospectively studied. Patients were randomly allocated to receive intrathecally either 10 mg isobaric bupivacaine plus 5 µg dexmetedomidine (group D n = 38) or 10 mg isobaric bupivacaine plus 25 mg fentanyl (group F n = 38), the onset time to reach peak sensory and motor level, the regression time for sensory and motor block, hemodynamic changes, and side effects were recorded. Results: Patients in group D had significant longer sensory and motor block times than patients in group F. the mean time of sensory regression to S1 was 274±73 min in group D and 179±47 min in group F (P < 0.001). The regression time of motor block to reach modified Bromage 0 was 240±60 min in group D and 155±46 min in group F (P< 0.001). The onset times to reach T10 dermatome and to reach peak sensory level as well as onset time to reach modified Bromage 3 motor block were not significantly different between the two groups. Conclusion: In women undergoing vaginal reconstructive surgery under spinal analgesia, 10 mg plain bupivacaine supplemented with 5 µg dexmetedomidine produces prolonged motor and sensory block compared with 25 µg fentanyl.

Two series of aldose N-(3-substituted-4-oxo-3,4-dihydroquinazolin-2-yl)hydrazones were prepared by the reaction of each of the aldoses with the appropriate 2-hydrazino-3-substituted-quinazolin-4(3H)-ones. Oxidative cyclisation of these aldose hydrazones with ferric chloride in ethanol yielded the title acyclo C-nucleosides.

Azolopyrimidines are biologically interesting molecules as indicated by the large number of recent papers dealing with synthesis, chemistry, and pharmacology of these molecules [1 – 9]. For example, zaleplon (1), a pyrazolopyrimidine, is a hypnotic agent licensed for treatment of insomnia [10], and allopurine (2), a 4-hydroxypyrazolopyrimidine used in the treatment of hyperuricemia and gout, inhibits de novo purine biosynthesis and xanthine oxidase [11] (Fig. 1). The triazolopyrimidine trapidil and its derivatives are coronary vasodilating and potential antiatherosclerotic drugs [12 – 14]. Also, pyrimidobenzimidazoles have been found to be of pharmacological interest; for example, pyrimido[1,2-a]benzimidazoles have been described as anti-hypertensive [15], anti-diabetic [16] and anti-inflammatory [17].

Coronary artery bypass grafting with cardiopulmonary bypass can induce systemic inflammatory response syndrome. To assess the prevalence of preoperative antithrombin and protein C deficiencies in relation to the incidence of this syndrome, antithrombin and protein C levels were measured in 130 patients undergoing coronary artery bypass grafting with cardiopulmonary bypass. Systemic inflammatory response syndrome developed in 36 (27.7%) patients who were predominantly male, had a lower EuroSCORE, longer cardiopulmonary bypass time, higher pre-bypass temperature, and shorter activated coagulation time. Logistic regression showed that predictive factors included bypass duration and pre-bypass temperature; however, low antithrombin levels appeared to be a negative predictive factor. Antithrombin levels were < 80% in 33.8% of patients, and 11.6% had protein C levels < 80%. Postoperative antithrombin and protein C deficiencies are not uncommon in adults undergoing cardiac surgery with cardiopulmonary bypass, but detection of these deficits did not identify patients at increased risk of systemic inflammatory response syndrome.

BACKGROUND: The present study was designed to assess whether an intraoperative administration of dexmedetomidine would decrease the intraoperative and postoperative analgesic requirements for paediatric patients undergoing hypospadius surgery. METHODS: Forty-eight children (American Society of Anesthesiologists-1) aged 1-12 years undergoing hypospadius repair under general anaesthesia were randomly assigned into dexmedetomidine or placebo groups, D and P, respectively. Group D received a loading dose of dexmedetomidine 1 microg kg(-1) after induction of anaesthesia, followed by a continuous infusion at a rate of 0.7 microg kg(-1) h(-1). Group P received a volume-matched 0.9% saline. Both groups received fentanyl for intraoperative analgesia and intravenous morphine and oral paracetamol for postoperative analgesia. For both groups, heart rate, blood pressure and fentanyl requirements were recorded intraoperatively. During their stay for 2 h in the recovery room, heart rate, blood pressure, pain scores, behaviour scores and total morphine requirements were recorded. After discharge from postanaesthesia care unit, paracetamol requirements over 24 h were also recorded. RESULTS: Intraoperatively, the dexmedetomidine-treated group had significantly fewer fentanyl requirements, slower heart rate and lower mean arterial blood pressure (P < 0.001). In the postanaesthesia care unit, this group also consumed significantly less morphine, had lower pain scores, lower behaviour score in the immediate postoperative period, lower heart rates and mean arterial blood pressures when compared with the placebo group (P < 0.001). Group D consumed significantly less paracetamol than group P in the ward over 24 h. CONCLUSION: Intravenous administration of dexmedetomidine intraoperatively during hypospadius repair in children reduces intraoperative and postoperative analgesic requirements and lowers heart rate and blood pressure.

Two series of aldose N-(3-substituted-4-oxo-3,4-dihydroquinazolin-2-yl)hydrazones were prepared by the reaction of each of the aldoses with the appropriate 2-hydrazino-3-substituted-quinazolin-4(3H)-ones. Oxidative cyclisation of these aldose hydrazones with ferric chloride in ethanol yielded the title acyclo C-nucleosides.

Some new pyrazole-5-carbonitrile derivatives 8, 9 and pyrazole-5-carboxamide 13 were synthesized by the cycloaddition reaction of nitrilimines 3, 4 to α-cyanocinnamonitriles 5a-f and α-cyanocinnamamide 12a, b respectively. On the other hand 3, 4 add to ethyl α-cyanocinnamate 14a-f to give ethyl 2-pyrazoline-5-carboxylate derivatives 15, 16. Also, cycloaddition of 3, 4 to 3-cyanocoumarin 19a or 3-phenylsulphonylcoumarin 19b or 3-bromocoumarin 19c give chromeno[3,4-c]pyrazol-4(3H)-one derivatives 20. In the same direction, the cycloaddition of 3, 4 to 3-acetylcoumarin 22 and 3-benzoylcoumarin 23 gives the corresponding dihydrochromeno[3,4-] pyrazol-4(3H)-one 24 and 25 respectively. Oxidation of 24 and 25 give 20. Most of the prepared compounds showed good to moderate antibacterial and antifungal activities. Alguns novos derivados de pirazol-5-carbonitrila 8, 9 e pirazol-5-carboxamida 13 foram sintetizados pela reação de cicloadição de nitriliminas 3, 4 a α-cianocinamonitrilas 5a-f e α-cianocinamamida 12a, b, respectivamente. Por outro lado, a adição de 3, 4 a α-cianocinamato de etila 14a-f leva à produção de derivados de 2-pyrazoline-5-carboxilato de etila, 15, 16. Também, a cicloadição de 3, 4 à 3-cianocumarina 19a ou à 3-fenilsulfonilcumarina 19b ou à 3-bromocumarina 19c leva à produção de derivados do cromeno[3,4-c]pirazol-4(3H)-ona, 20. A cicloadição de 3, 4 à 3-acetilcumarina, 22 e 3-benzoilcumarina, 23, produz o correspondente diidrocromeno[3,4-c]pirazol-4(3H)-ona, 24 e 25, respectivamente. A oxidação de 24 e 25 produz 20. A maioria dos compostos preparados mostrou boa a moderada atividade antibacteriana e antifúngica.

Azolopyrimidines are biologically interesting molecules as indicated by the large number of recent papers dealing with synthesis, chemistry, and pharmacology of these molecules [1 – 9]. For example, zaleplon (1), a pyrazolopyrimidine, is a hypnotic agent licensed for treatment of insomnia [10], and allopurine (2), a 4-hydroxypyrazolopyrimidine used in the treatment of hyperuricemia and gout, inhibits de novo purine biosynthesis and xanthine oxidase [11] (Fig. 1). The triazolopyrimidine trapidil and its derivatives are coronary vasodilating and potential antiatherosclerotic drugs [12 – 14]. Also, pyrimidobenzimidazoles have been found to be of pharmacological interest; for example, pyrimido[1,2-a]benzimidazoles have been described as anti-hypertensive [15], anti-diabetic [16] and anti-inflammatory [17].

A series of α-azidoglyoxatic acid anilide arylhydrazones 2 were prepared and converted to the corresponding phosphonimines 6 by reaction with triphenylphosphine. Treatment of the latter with acyl chlorides yielded the phosphonium salts 9 which afforded, upon treatment with triethylamine, 1, 5-disubstituted 1H-1, 2, 4-triazole-3-carboxylic acid anilides 11. Acid hydrolysis of 6 yielded the amidrazones 8.

The chemistry of isoquinolines has always been of considerable interest [1 – 5]. A large number of isoquinolines have important pharmacological applications as anesthetics (1), antihypertension agents like quinapril, quinaprilate and debrisoquine, antifungal agents such as 2,2′-hexadecamethylenedisoquinolinium dichloride (2), disinfectants like N-laurylisoquinolinium bromide (3) and vasodilators, with the well-known example of papaverine (4) (Fig. 1) [6 – 9].

Periosteal chondromas (juxtacortical chondromas), are slow growing, rare cartilaginous lesion that arises adjacent to the cortex beneath the periosteum. They occur more in males in their 20s. We report a rare case of periosteal chondroma arising from the left clavicle of a 56year old male. We could only find one reported case in the English literature of periosteal chondroma arising from the research and to the best of our knowledge, this is the second reported case.