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Synthesis, admetSAR Predictions, DPPH Radical Scavenging Activity, and Potent Anti-mycobacterial Studies of Hydrazones of Substituted 4-(anilino methyl) benzohydrazides (Part 2)

Author(s):

Vijay J. Desale, Suraj N. Mali, Bapu R. Thorat* and Ramesh S. Yamgar   Pages 1 - 11 ( 11 )

Abstract:


Background: For the past several decades, we are remarking presence of the tuberculosis (TB) as the most common infectious disease leading mortality.

Objective: 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.

Results: 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.

Conclusion: Our current study revealed promising in-vitro antituberculosis and antioxidant profiles of hydrazidehydrazone analogues.

Keywords:

hydrazide-hydrazones, Anti-oxidant activity, Anti-tuberculosis activity, in-silico analysis, tuberculosis, synthesis

Affiliation:

P.G. and Research Centre, Department of Chemistry, Government of Maharashtra’s Ismail Yusuf College, Jogeshwari, Mumbai-400060, Government College of Pharmacy, Karad, Maharashtra, P.G. and Research Centre, Department of Chemistry, Government of Maharashtra’s Ismail Yusuf College, Jogeshwari, Mumbai-400060, Department of Chemistry, PatkarVarde College of Arts, Science and Commerce, Goregaon (W), Mumbai 400 062



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