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

Abstract

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.

The Material Basis and Mechanism of Xuefu Zhuyu Decoction in Treating Stable Angina Pectoris and Unstable Angina Pectoris

“…In contrast to forward network pharmacology, the reverse network pharmacology approach allows for the reverse access to the targets and components at play in the complex networks constructed from the perspective of disease characterization and function [ 16 ]. The strength of binding of a compound to different targets can be expressed in terms of the results of molecular docking [ 17 , 18 ]. Furthermore, a range of compounds in a prescription can be docked to target proteins of different diseases to reveal the therapeutic characteristics of the prescription for different diseases.…”

Greener Synthesis, In-Silico and Theoretical Analysis of Hydrazides as Potential Antituberculosis Agents (Part 1)

“…Antimicrobial resistance is a severe global healthcare threat, which is hampering the quality of human life [1][2][3][4]. Searching for potent, safe, and effective agents is still a difficult task for medicinal chemists all over the world.…”

“…Searching for potent, safe, and effective agents is still a difficult task for medicinal chemists all over the world. Tuberculosis (TB) remains a major global healthcare threat, as reported in WHO in 2019 [4]. Hydrazide-hydrazones motifs were reported for their wider pharmacological potentials, such as being anticonvulsant, anticancer, antiviral, etc.…”

“…Hydrazide-hydrazones motifs were reported for their wider pharmacological potentials, such as being anticonvulsant, anticancer, antiviral, etc. [4]. Recently, computational methodologies are also gaining tremendous attention by medicinal chemists .…”

A Chitosan Hydrochloride Mediated, Simple and Efficient Approach for the Synthesis of Hydrazones, their in vitro Antimycobacterial Evaluations, and Molecular Modeling Studies (Part III)

“…39 From our previous report, we used Chitosan Hydrochloride successfully to synthesis newer set of hydrazones. 40 Moreover, from our previous medicinal chemistry knowledge [41][42][43][44][45][46][47][48][49] on hydrazones as antitubercular agents (anti-TB) agents, we noticed that these moieties particularly represented strong anti-TB activities, typically MICs (minimum inhibitory concentrations) ranging from (1.25-100 µg/mL). In continuation of same, we further extended our work to synthesis a set of hydrazones with a catalyst, Chitosan hydrochloride.…”