Benzylsulfanyl Benzo-heterocycle Amides and Hydrazones As New Agents Against Drug-susceptible and Resistant

Overview

Journal Medchemcomm

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2018 Aug 16

PMID 30108841

Citations 1

Authors

Xiaoyun Lu

Xianglong Hu

Zhiyong Liu

Tianyu Zhang

Ruibing Wang

Baojie Wan

Scott G Franzblau

Qidong You

Affiliations

Soon will be listed here.

Abstract

A series of benzylsulfanyl benzo-heterocycle amides and hydrazones were synthesized and evaluated for anti-tubercular activities. The isonicotinyl hydrazone derivatives , and exhibited good anti-tubercular activity against HRv (ATCC #27294) with MIC values of 0.23, 0.24 and 0.24 μM, respectively, and were also active against SDR-TB, MDR-TB and XDR-TB. More importantly, compound also showed low cytotoxicity and good metabolic stability, and could significantly reduce the mycobacterial burden in a mouse model infected with autoluminescent H37Ra strain, which may serve as a lead compound for further development.

Citing Articles

Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds.

Dos Santos Fernandes G, Chin C, Dos Santos J Pharmaceuticals (Basel). 2017; 10(2).

PMID: 28587160 PMC: 5490408. DOI: 10.3390/ph10020051.

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