Identification of a novel class of quinoline-oxadiazole hybrids as anti-tuberculosis agents

被引：48

作者：

Jain, Puneet P. ^{[1
]}

Degani, Mariam S. ^{[1
]}

Raju, Archana ^{[1
]}

Anantram, Aarti ^{[1
]}

Seervi, Madhav ^{[1
]}

Sathaye, Sadhana ^{[1
]}

Ray, Muktikanta ^{[2
]}

Rajan, M. G. R. ^{[2
]}

机构：

[1] Inst Chem Technol, Bombay 400019, Maharashtra, India

[2] Tata Mem Hosp, Radiat Med Ctr, Bombay 400012, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 02期

关键词：

Mycobacterium tuberculosis; Isosterism; Oxadiazole; Quinoline; Bedaquiline; MICROTITER ASSAY PLATE; MYCOBACTERIUM-TUBERCULOSIS; INEXPENSIVE METHOD; DRUG DISCOVERY; DESIGN; INHIBITORS; 1,2,4-OXADIAZOLES; DERIVATIVES; MOLECULES; ACIDS;

D O I：

10.1016/j.bmcl.2015.11.057

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel quinoline-oxadiazole hybrid compounds was designed based on stepwise rational modification of the lead molecules reported previously, in order to enhance bioactivity and improve druglikeness. The hybrid compounds synthesized were screened for biological activity against Mycobacterium tuberculosis H(37)Rv and for cytotoxicity in HepG2 cell line. Several of the hits exhibited good to excellent anti-tuberculosis activity and selectivity, especially compounds 12m, 12o and 12p, showed minimum inhibitory concentration values < 0.5 mu M and selectivity index >500. The results of this study open up a promising avenue that may lead to the discovery of a new class of anti-tuberculosis agents. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：645 / 649

页数：5

共 29 条

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