Tuberculosis (TB) is a major cause of mortality and illness as reported by the 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 synthesise more potent hydrazide–
hydrazones, containing anti-tubercular agents.
Methods: In the current study, we 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, ultraviolet–visible spectroscopy, fluorescence, fourier-
transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. 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. The hydrazide CO-NH protons in (3a-j) compounds are highly deshielded and showed
broad singlet at 9.520-9.168 ppm. All the compounds were found to have more intense emission in
the 416 – 429 nm regions and strong absorption in the regions of 316 – 327 nm. Synthesized compounds
were also tested for in silico analysis using different software for their Absorption, Distribution,
Metabolism, Excretion and Toxicity (ADMET) analysis. All the compounds were found to be
in silico non-carcinogenic.
Conclusion: It will be worth saying that our in silico and in vitro approaches used in the current
study will become a guide for medicinal chemists to make structural modifications and synthesize
more effective and potent hydrazone containing anti-tubercular agents.