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Synthesis, In-silico and In-vitro Analysis of Hydrazones as Potential Antituberculosis Agents

Author(s):

Bapu R. Thorat*, Suraj Mali, Deepa Rani and Ramesh Yamgar   Pages 1 - 12 ( 12 )

Abstract:


Tuberculosis (TB) is remaining a major cause of mortality and illness as reported by W.H.O in 2019. The WHO report also mentioned the fact that about 10.0 million people fell ill with tuberculosis in the year 2018. Hydrazide–hydrazones having azomethine group (–NH–N=CH–) connected with carbonyl group is reported for the number of bioactivities like anti-inflammatory, anticonvulsant, anticancer, antiviral and antiprotozoal.

Objective: The objective of our current study is to design and synthesis of more potent Hydrazide–hydrazones containing anti-Tubercular agents.

Methods: In the current study, we have synthesized 10 hydrazones (3a-3j) by stirring corresponding benzohydrazides (2) with substituted aldehydes (1a-j) in ethanol as a solvent and acetic acid as a catalyst at room temperature. All synthesized compounds were characterized by various spectroscopic techniques including Elemental analysis, UV, Fluorescence, FT-IR and 1H-NMR. Compounds (3a-3j) were tested for in-vitro anti-TB activity using Microplate Alamar Blue assay (MABA).

Results: All our synthesized compounds (3a-3j) were found to be potent against Mycobacteria tuberculosis (H37RV strain) with MIC (minimum inhibitory concentrations) values of 3.125-50 µg/mL. Synthesized compounds were also tested for in-silico analysis using diffent softwares for their Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) analysis.

Conclusion: Our current study will definitely help the medicinal chemists for better designing of newer potent anti-Tubercular agents.

Keywords:

Hydrazide-hydrazones, Antituberculosis activity, In-silico analysis, Tuberculosis, Synthesis

Affiliation:

Department of Chemistry, Government of Maharashtra’s Ismail Yusuf College of Arts, Science and Commerce, Department of Pharmaceutical Sciences, Government College of Pharmacy, Karad, Department of Chemistry, Government of Maharashtra’s Ismail Yusuf College of Arts, Science and Commerce, Mumbai 60, Department of Chemistry, Chikitsak Samuha’s Patkar-Varde College of Arts, Science and Commerce, Goregaon (West), Mumbai 400 062



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