ascorbic-acid has been researched along with 1-2-4-triazole* in 2 studies
2 other study(ies) available for ascorbic-acid and 1-2-4-triazole
| Article | Year |
|---|---|
Synthesis and biological activities of some novel aminomethyl derivatives of 4-substituted-5-(2-thienyl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones.
A novel series of compounds were synthesized by cyclic condensation reaction of substituted isothiocyanate (2a-c) with 2-thiophenecarboxylic acid hydrazide (1) in the presence of ethyl alcohol, to obtain intermediate thiosemicarbazides (3a-c), which were further treated with sodium hydroxide in the presence of ethanol to obtain triazole derivatives (4a-c). The latter were refluxed with substituted secondary amines and formaldehyde for 6-10 h to afford Mannich bases (5a-k). The synthesized compounds were characterized on the basis of their spectral (IR, (13)C and (1)H NMR) data and evaluated for biological activities. Some of the compounds were found to exhibit significant antimicrobial and antioxidant activity. Topics: Anti-Bacterial Agents; Antifungal Agents; Antioxidants; Aspergillus flavus; Aspergillus fumigatus; Biphenyl Compounds; Dose-Response Relationship, Drug; Escherichia coli; Free Radical Scavengers; Microbial Sensitivity Tests; Models, Chemical; Molecular Structure; Oxidation-Reduction; Penicillium; Picrates; Staphylococcus aureus; Thiones; Triazoles; Trichophyton | 2013 |
Novel 1,2,4-triazole and imidazole derivatives of L-ascorbic and imino-ascorbic acid: synthesis, anti-HCV and antitumor activity evaluations.
Several novel 1,2,4-triazole and imidazole L-ascorbic acid (1, 2, 3, 5, 6 and 9) and imino-ascorbic acid (4, 7 and 8) derivatives were prepared and evaluated for their inhibitory activity against hepatitis C virus (HCV) replication and human tumour cell proliferation. Compounds 6 and 9 exerted the most pronounced cytostatic effects in all tumour cell lines tested, and were highly selective for human T-cell acute lymphoblastic leukaemia cells (CEM/0) with IC(50)s of 10 ± 4 and 7.3 ± 0.1 μM, respectively. Unlike compound 9, compound 6 showed no toxicity in human diploid fibroblasts. One of the possible mechanisms of action of compound 6 accounting for observed cytostatic activity towards haematological malignancies might be inhibition of inosine monophosphate dehydrogenase (IMPDH) activity, a key enzyme of de novo purine nucleotide biosynthesis providing the cells with precursors for DNA and RNA synthesis indispensable for cell growth and division, which has emerged as an important target for antileukemic therapy. In addition, this compound proved to be the most potent inhibitor of the hepatitis C virus replication as well. However, observed antiviral effect was most likely associated with the effect that the compound exerted on the host cell rather than with selective effect on the replication of the virus itself. In conclusion, results of this study put forward compound 6 as a potential novel antitumor agent (IMPDH inhibitor) for treating leukaemia. Its significant biological activity and low toxicity in human diploid fibroblasts encourage further development of this compound as a lead. Topics: Animals; Antineoplastic Agents; Antiviral Agents; Ascorbic Acid; Cell Line, Tumor; Dogs; Drug Evaluation, Preclinical; Drug Screening Assays, Antitumor; Fibroblasts; Hepacivirus; Humans; Imidazoles; IMP Dehydrogenase; Magnetic Resonance Spectroscopy; Molecular Structure; Triazoles; Virus Replication | 2012 |