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Application of two coformers, l-tartaric acid (TA) and ascorbic acid (AA) was evaluated on the solubility of pioglitazone hydrochloride (PGZ.HCl). Solid dispersions were prepared using the solvent evaporation method. Drug solubility was evaluated in bio-relevant media and the results were compared to the physical mixtures (PM) of the drug + coformer, and the pure drug. Physicochemical characterisation of the developed products was characterised using Fourier transformation-infrared spectroscopy (FT-IR), Differential scanning calorimeter (DSC), and X-ray powder diffractometry (XPRD). Physical mixtures of PGZ-AA (PM) were able to enhance drug solubility to the same extent as the solvent evaporation method (PGZ-AA). This indicates that the preparation process has little effect on drug solubility. Up to 7-fold enhancement was observed for drug solubility in distilled water and buffer pH 1.2. Physical mixtures seem more feasible method to significantly enhance drug solubility without the need to use toxic solvents and time-consuming evaporation methods. [ABSTRACT FROM AUTHOR]

Objective: Unfortunately, infectious diseases are still one of the most important health problems around the world. The resistance of pathogenic bacteria to several drugs is an important and growing problem in the treatment of infectious diseases and hospital infections. It seems necessary to identify new compounds that have inhibitory or lethal effects on this bacterium. That's why we decided antimicrobial efficacy. The newly synthesized compound (2-methyl-1,3-dioxo-',11',2',3',5',6',7'a,7-octahydrospiro] inden-'2,3-pyrrolizidine 2-carboxylate (5) on Staphylococcus aureus and Escherichia coli bacteria. Methods: At first, synthesized of methyl'2-methyl-1,3-dioxo-1',1',2',3',5',6', 7',7'a, -octahydrospiro] inden-'2,3-pyrrolizidine 2-Carboxylate was prepared by green chemistry method and with the help of microwave in one pot. Microbial culture media containing control bacteria of Staphylococcus aureus and Escherichia coli were prepared and concentrations of 70 to 110 Landa of the above compound were added to the samples. The antimicrobial property of the samples was determined after 3 days using the disk diffusion method and broth micro dilution method was determined, as well as the minimum inhibitory concentration and bacterial lethality of the samples Results: The minimum inhibitory concentration and bacterial lethality in the above combination against the same standard strain of Escherichia coli bacteria was obtained at the rate of 12.5 µg/mL. The minimum inhibitory and lethal concentration of methyl methacrylate compound against the standard strain of Staphylococcus aureus bacteria was 12.5 and 25 µg/mL, respectively. Conclusion: The use of the above combination was effective in controlling and inhibiting the tested bacteria. [ABSTRACT FROM AUTHOR]

Experimental solubility of dexamethasone was obtained in binary aqueous mixtures of ethanol, methanol and acetonitrile at 298.2 K. The effects of micellization and pH were also investigated on the solubility of the drug. Experimental solubility data in the binary solvent mixtures were correlated by three co-solvency models, i.e. Yalkowsky, CNIBS/R-K, and the modified Wilson model. A new principle has also been investigated with the purpose of modelling drug solubility in the binary solvent mixtures using Polarised Continuum Model (PCM) by using the hybrid functional B3LYP method and 6–311++G** basis set. By matching experimental data with PCM modelling, we investigated the outcome of drug solubility in various mass fractions of binary solvent mixtures. Here we report the solute-solvent interaction energy as free energy of solvation (∆Gsol), total electrostatic energy, dipole moment, total Gibbs-free energy and dielectric constant (ε) of dexamethasone in various mass fractions of ethanol + water mixtures. [ABSTRACT FROM AUTHOR]

Minoxidil (2,4-diamino-6-piperidinopyrimidine 3-oxide) was primarily recognized as a drug for reducing vascular resistance to blood flow. It was later introduced as a more important medicine for topical stimulation of hair growth and baldness reverting as well as treatment of androgenic alopecia through increasing prostaglandin endoperoxide synthesis. In this study, magnetic nanoparticles (MNPs) of spinel ferrites (MFe2O4 , M = Co, Ni, Fe, Cu, and Zn) via solid-state grinding procedure were prepared and then characterized using X-ray diffraction, scanning electron microscopy, transmission electron microscopy, vibrating sample magnetometer, and Fourier transform infrared techniques. The prepared nanoferrites were utilized as efficient and green heterogeneous catalysts for N -oxidation of 2,6-diamino-4- chloro-pyrimidine with H2O2 in refluxing ethanol giving 2,6-diamino-4-chloro-pyrimidine N -oxide as a starting material for the synthesis of 2,4-diamino-6-piperidinopyrimidine 3-oxide (minoxidil). Among the examined nanoferrites, CoFe2O4 MNPs exhibited prominent catalytic activity giving the product in 95% yield within 60 min. Moreover, the reusability of nano-CoFe2O4 was examined for 6 consecutive cycles without significant loss of catalytic activity and magnetic property. [ABSTRACT FROM AUTHOR]

NaBH3CN as a modified hydroborate agent and due to a strong withdrawing CN group does not show any reducing ability to reduce functional groups in the absence of acidic media (pH ~ 3–4). In this study, the immobilized sulfonic acid on silica, SiO2@SO3H, was prepared and applied as a new solid acid catalyst for extremely enhancing the reducing ability of NaBH3CN. The influence of SiO2@SO3H was highlighted by performing the quick and green reduction of structurally diverse carbonyl compounds involving aldehydes, ketones, α,β‐unsaturated enals and enones, α‐diketones, and acyloins to the corresponding alcohols or alkanes with NaBH3CN. By the NaBH3CN/SiO2@SO3H system, aldehydes were reduced to the corresponding alcohols and ketonic compounds to alkanes as reductive‐deoxygenation products. All reduction reactions were carried out within 3 min at room temperature and under solvent‐free conditions to afford the products in high to excellent yields (90–98%). The immobilized sulfonic acid on silica, SiO2@SO3H, was prepared and applied for extremely enhancing the reducing ability of NaBH3CN. The influence of SiO2@SO3H was highlighted by performing the quick and green reduction of structurally diverse carbonyl compounds to alcohols or alkanes with NaBH3CN. By the NaBH3CN/SiO2@SO3H system, aldehydes were reduced to the corresponding alcohols and ketones to alkanes as reductive‐deoxygenation products. [ABSTRACT FROM AUTHOR]

Background and Objectives: Bacterial resistance is an emerging public health problem worldwide. Metallic nanoparticles and nanoalloys open a promising field due to their excellent antimicrobial effects. The aim of the present study was to investigate the antibacterial effects of Ag-Cu nanoalloys, which were biosynthesized by Lactobacillus casei ATCC 39392, on some of the important bacterial pathogens, including Escherichia coli, Burkholderia cepacia, Listeria monocytogenes and Brucella abortus. Materials and Methods: Ag-Cu nanoalloys were synthesized through the microbial reduction of AgNO3 and CuSO4 by Lactobacillus casei ATCC39392. Furthermore, they were characterized by Fourier-Transform Infrared Spectrometer (FTIR) and Field Emission Scanning Electron Microscopy (FESEM) analysis in order to investigate their chemical composition and morphological features, respectively. The minimum inhibitory and minimum bactericidal concentrations of Ag-Cu nanoalloys were determined against each strain. The bactericidal test was conducted on the surface of MHA supplemented with 1, 0.1, and 0.01 µg/µL of the synthesized nanoalloy. The antimicrobial effects of synthesized nanoalloy were compared with ciprofloxacin, ampicillin and ceftazidime as positive controls. Results: Presence of different chemical functional groups, including N-H, C-H, C-N and C-O on the surface of Ag-Cu nanoalloys was recorded by FTIR. FESEM micrographs revealed uniformly distributed nanoparticles with spherical shape and size ranging from 50 to 100 nm. The synthesized Ag-Cu nanoalloys showed antibacterial activity against L. monocytogenes PTCC 1298, E. coli ATCC 25922 and B. abortus vaccine strain. However, no antibacterial effects were observed against B. cepacia ATCC 25416. Conclusion: According to the findings of the present research, the microbially synthesized Ag-Cu nanoalloy demonstrated antibacterial effects on the majority of the bacteria studied even at 0.01 µg/µL. However, complementary investigations should be conducted into the safety of this nanoalloy for in vivo or systemic use. [ABSTRACT FROM AUTHOR]

One-pot cyclocondensation reaction of ninhydrin, proline and acrylates/1,4- naphthoquinone produces some novel highly diastereo- and regioselective octahydrospiro[indene- 2,3'-pyrrolizidine]-1,3-diones in 81-95% yields. The reactions are carried out in ethanol at room temperature, refluxand microwave irradiation through the initial formation of azomethineylide intermediate. [ABSTRACT FROM AUTHOR]