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Current Computer-Aided Drug Design

Author(s): Vijay J. Desale, Suraj N. Mali, Hemchandra K. Chaudhari, Maya C. Mali, Bapu R. Thorat* and Ramesh S. Yamgar

DOI: 10.2174/1573409915666191018120611

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Synthesis and Anti-mycobacterium Study on Halo-substituted 2-aryl oxyacetohydrazones

Page: [618 - 628] Pages: 11

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Abstract

Background: The treatment of multiple-drug-resistant tuberculosis (MDR-TB) with currently available marketed drugs remains a global health concern. The cases of resistant tuberculosis patients are increasing day by day.

Objective: The objective of this study is to highlight the need of developing shorter, simpler and tolerable drug regimens.

Methods: In the present study, we synthesized various halo-substituted 2-aryloxyacetohydrazones via a series of reactions from halo-substituted phenols. All the compounds were characterized by using various spectroscopic methods, such as NMR, FT-IR, UV spectroscopy, etc.

Results: All the synthesized hydrazones showed theoretically good interactions with enzyme enoyl reductase (pdb id: 4tzk). All the synthesized compounds (5a-5o) showed moderate to good activity (3.125-100 μg/mL) against Mycobacteria tuberculosis, H37RV strain.

Conclusion: Our results would pave a new way for the development of more effective Anti-TB agents in the future.

Keywords: 2-aryloxyacetohydrazones, hydrazones, Anti-TB activity, molecular docking, Mycobacteria tuberculosis, enoyl reductase.

Graphical Abstract

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