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

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

Journal Name: Current Computer-Aided Drug Design

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

Objective: There is a need to develop shorter, simpler and tolerable drug regimens.

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

Results: All the synthesized hydrazones were 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 definitely pave the new way towards development of more effective Anti-TB agents in future.

Keywords: 2-aryloxyacetohydrazones, Hydrazones, Anti-TB activity, Molecular Docking, Mycobacteria tuberculosis

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(E-pub Ahead of Print)
DOI: 10.2174/1573409915666191018120611
Price: $95

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