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

[ Vol. 16 , Issue. 5 ]

Author(s):

Vijay J. Desale, Suraj N. Mali, Hemchandra K. Chaudhari, Maya C. Mali, Bapu R. Thorat* and Ramesh S. Yamgar   Pages 618 - 628 ( 11 )

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.

Affiliation:

Department of Chemistry, N.B. Mehta Science College, Bordi, Dist. Palghar-401701, Maharashtra, Department of Pharmaceutical Sciences, Institute of Chemical Technology, Matunga, Mumbai 400019, Department of Pharmaceutical Sciences, Institute of Chemical Technology, Matunga, Mumbai 400019, Department of Pharmaceutical Sciences, Institute of Chemical Technology, Matunga, Mumbai 400019, Faculty of P.G. and Research Centre, Department of Chemistry, Government of Maharashtra’s Ismail Yusuf College, Jogeshwari, Mumbai-400060, Department of Chemistry, Patkar-Varde College of Arts, Science and Commerce, Goregaon (W), Mumbai 400 062

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