Synthesis, Spectroscopic, In-vitro and Computational Analysis of Hydrazones as Potential Antituberculosis Agents: (Part-I)

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Author(s): Bapu R. Thorat*, Deepa Rani, Ramesh S. Yamgar, Suraj N. Mali.

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

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Background: Since last decades, the healthcare sector is facing the problem of development of multidrug-resistant (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) infections all over the world. Regardless of current healthcare progress for treatment of mycobacterial infections, we are still unable to control addition of every year 9 million new cases of tuberculosis (TB).

Objective: We had objective to synthesize some novel hydrazones, which were further subjected to characterization, Photoluminescence study, in-vitro anti-mycobacterium testing and in-silico ADMET predictions.

Methods: Some new hydrazone derivatives have been successfully prepared by the condensation reaction in the present study. All the compounds were characterized by using FTIR, NMR, UV, Fluorescence spectroscopic techniques.

Results: All our newly synthesized compounds showed strong electronic excitation at 292.6 – 319.0 nm and displayed more intense emissions in the 348 – 365 nm regions except compound 3i. The newly synthesized hydrazones 3a, 3b, 3f and 3g were found to be most active compounds and showed MIC (Minimum inhibitory concentrations) values of 12.5 μg/mL.

Conclusion: In the realm of development of more potent, effective, safer and less toxic antituberculosis agents; our current study would definitely help the medicinal chemists to develop potent analogues containing hydrazine motifs in them.

Keywords: Hydrazide-hydrazones, antituberculosis activity, in-silico analysis, tuberculosis, synthesis, ADMET predictions.

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(E-pub Ahead of Print)
DOI: 10.2174/1386207323999200325125858
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