Vijay J. Desale, Suraj N. Mali, Bapu R. Thorat* and Ramesh S. Yamgar Pages 1 - 11 ( 11 )
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.
hydrazide-hydrazones, Anti-oxidant activity, Anti-tuberculosis activity, in-silico analysis, tuberculosis, synthesis
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