Title:Synthesis and Anti-mycobacterium Study on Halo-substituted 2-aryl oxyacetohydrazones
VOLUME: 16 ISSUE: 5
Author(s):Vijay J. Desale, Suraj N. Mali, Hemchandra K. Chaudhari, Maya C. Mali, Bapu R. Thorat* and Ramesh S. Yamgar
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
Keywords:2-aryloxyacetohydrazones, hydrazones, Anti-TB activity, molecular docking, Mycobacteria tuberculosis, enoyl reductase.
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.
