ascorbic-acid and pyrazole

New candidates of 3-(4,5-dihydro-1H-pyrazol/isoxazol-5-yl)-2-phenyl-1H-indole derivatives (4-7) were designed combining the pyrazoline/isoxazoline heterocycles and 2-phenylindole to explore its potential as 15-lipoxygenase (15-LOX) inhibitors. The design of the new derivatives was based on utilizing the antioxidant properties of pyrazoline, 2-phenylindole and the good 15-LOX inhibition properties of indolylpyrazoline. The derivatives were synthesized adopting simple and laboratory friendly reaction conditions to give the target compounds in quantitative yields. The resulting indolylpyrazolines/isoxazolines were evaluated as antioxidants against 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and superoxide dismutase (SOD); indolylpyrazoline (4b) was the most potent antioxidant against SOD assay (IC

Topics: Androstenols; Antioxidants; Arachidonate 15-Lipoxygenase; Dose-Response Relationship, Drug; Drug Design; Glycine max; Humans; Indoles; Lipoxygenase Inhibitors; Molecular Docking Simulation; Molecular Structure; Pyrazoles; Structure-Activity Relationship

A series of novel pyrazole integrated benzophenones (9a-j) have been designed, synthesized from 1-methyl-5-(2,4,6-trimethoxy-phenyl)-1H-pyrazole 6. The structures of the regioisomers 6 and 7 were determined by 2D (1)H-(1)H COSY, (1)H-(13)C HSQC and (1)H-(13)C HMBC experiments. The newly synthesized compounds (9a-j) were evaluated for in vivo anti-inflammatory activity by carrageenan paw edema in rats and in vitro COX-1/COX-2 inhibition and antioxidant potential. Among the synthesized compounds, compounds 9b, 9d and 9f, were found to be active anti-inflammatory agents in addition to having potent antioxidant activity.

Topics: Animals; Anti-Inflammatory Agents; Antioxidants; Benzophenones; Cells, Cultured; Drug Design; Enzyme Activation; Enzyme Inhibitors; Pyrazoles; Rats; Stereoisomerism

This study has achieved the design and diversity-oriented synthesis of novel 1,4-thiazepine derivatives embedded with carbazole, pyrazole or isoxazole motif via microwave-assisted multicomponent reactions under solvent-free condition, thus providing a green and facile access to 1,4-thiazepine derivatives with prominent features of high structural diversity, short reaction time, high yields and environmental friendliness. More importantly, these novel compounds have been subjected to the test of in vitro antioxidant and cytotoxic activities, resulting in the finding that these 1,4-thiazepine derivatives not only have significant antioxidant activity, but also exhibit remarkably selective cytotoxicity to carcinoma cell line HCT 116.

Topics: Antineoplastic Agents; Antioxidants; Carbazoles; Cell Line, Tumor; Chemistry, Pharmaceutical; Drug Design; Drug Screening Assays, Antitumor; HCT116 Cells; Humans; Microwaves; Models, Chemical; Pyrazoles; Solvents; Temperature; Thiazepines

In the present study, we have synthesized novel dihydropyrimidines (1a-j), their dimethylated adducts (2a-j), and hydrazine derivatives (3a-j) of 2a-j and subsequently their pyrazole derivatives (4a-j). Elemental analysis, IR, 1H NMR and mass spectral data elucidated structure of newly synthesized compounds. Some of these novel derivatives showed moderate to potent in vitro antioxidant, anti-inflammatory, antibacterial, antifungal and anthelmintic activity.

Topics: Animals; Anthelmintics; Anti-Infective Agents; Anti-Inflammatory Agents, Non-Steroidal; Antioxidants; Bacteria; Drug Evaluation, Preclinical; Fungi; Microbial Sensitivity Tests; Molecular Structure; Oligochaeta; Pyrazoles; Pyrimidines; Stereoisomerism

An oxo-bridged diruthenium(III) complex containing pyrazolato and pyrazole ligands is stable against ascorbic-acid reduction, induces apoptosis (60%, 48 h) against HeLa cells at 10 microM level and exhibits promising anti-angiogenic activity at its sub-cytotoxic concentrations. Other mononuclear ruthenium(III) complexes containing pyrazole ligands [Ru(pz)(4)X(2)](+) exhibit dual anti-angiogenic and cytotoxic properties.

Topics: Angiogenesis Inhibitors; Apoptosis; Ascorbic Acid; Cell Line, Tumor; Coordination Complexes; Crystallography, X-Ray; Drug Screening Assays, Antitumor; HeLa Cells; Humans; Ligands; Molecular Conformation; Pyrazoles; Ruthenium

The presence of yeast cells in the incubation medium prevents the oxidation of ascrobate catalyzed by copper ions. Ethanol increases ascorbate retention. Pyrazole, an alcohol dehydrogenase inhibitor, prevents ascorbate stabilization by cells. Chelation of copper ions does not account for stabilization, since oxidation rates with broken or boiled cells or conditioned media are similar to control rates in the absence of cells. Protoplast integrity is needed to reach optimal values of stabilization. Chloroquine, a known inhibitor of plasma membrane redox systems, inhibits the ascorbate stabilization, the inhibition being partially reversed by coenzyme Q6. Chloroquine does not inhibit ferricyanide reduction. Growth of yeast in iron-deficient media to increase ferric ion reductase activity also increases the stabilization. In conclusion, extracellular ascorbate stabilization by yeast cells can reflect a coenzyme Q dependent transplasmalemma electron transfer which uses NADH as electron donor. Iron deficiency increases the ascorbate stabilization but the transmembrane ferricyanide reduction system can act independently of ascorbate stabilization.

Topics: Ascorbic Acid; Cell Membrane; Chloroquine; Electron Transport; Enzyme Inhibitors; Ethanol; Ferricyanides; Kinetics; NAD; NADH, NADPH Oxidoreductases; Oxidation-Reduction; Pyrazoles; Saccharomyces cerevisiae; Sulfhydryl Reagents; Ubiquinone

Topics: Animals; Ascorbic Acid; Dimethyl Sulfoxide; Ethanol; Fomepizole; Free Radicals; Hydroxides; Hydroxyl Radical; Kinetics; Male; Microsomes, Liver; Oxidation-Reduction; Pyrazoles; Rats; Rats, Inbred Strains; Xanthine Oxidase