Synthesis, admetSAR predictions, DPPH radical scavenging activity and potent anti-mycobacterial studies of hydrazones of substituted 4-(anilinomethyl)benzohydrazides (Part 2).

Clicks: 397
ID: 108588
2020
For the past several decades, we are remarking presence of the tuberculosis (TB) as the most common infectious disease leading mortality.Hydrazone containing azometine group (-NHN=CH-) compounds has been reported for broad range of bioactivities such as antiplatelet, analgesic, antiinflammatory, anticonvulsant, antidepressant, antimalarial, vasodilator , antiviral and antimicrobial, etc. Method: For synthesis of our compounds (4a-4d) and (6a-6e), we have treated aromatic amines with methyl terephthalaldehydate in methanol giving us Schiff's bases followed by reductive amination and further treatment with hydrazine hydrate to give acid hydrazides (4a-4d). These acid hydrazides were then treated with different aromatic aldehydes to yield hydrazones (6a-6d). All our synthesized compounds were subjected to FT-IR, NMR, and UV spectroscopic characterization.Compounds (4a-4d) and (6a-6e) were found to have highly potent activity against Mycobacteria tuberculosis (Vaccine strain, H37 RV strains): ATCC No- 27294 (MIC:1.6-6.25 μg/mL) than standard anti-TB drugs. Our compounds exhibited good radical scavenging potentials(0-69.2%) as checked from DPPH protocol. All compounds also demonstrated good in-silico ADMET results.Our current study revealed promising in-vitro antituberculosis and antioxidant profiles of hydrazidehydrazone analogues.
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desale2020synthesiscurrent Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Desale, Vijay J;Mali, Suraj N;Thorat, Bapu R;Yamgar, Ramesh S;
Journal current computer-aided drug design
Year 2020
DOI 10.2174/1573409916666200615141047
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