Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides

被引：16

作者：

Suman, Pathi ^{[1
]}

Dayakar, Cherupally ^{[1
]}

Rajkumar, Kommera ^{[1
]}

Yashwanth, Bomma ^{[2
]}

Yogeeswari, Perumal ^{[3
]}

Sriram, Dharmarajan ^{[3
]}

Rao, Janapala Venkateswara ^{[2
]}

Raju, Bhimapaka China ^{[1
]}

机构：

[1] CSIR, Indian Inst Chem Technol, Nat Prod Chem Div, Hyderabad 500007, Andhra Pradesh, India

[2] CSIR, Indian Inst Chem Technol, Div Biol, Hyderabad 500007, Andhra Pradesh, India

[3] Birla Inst Technol & Sci Pilani, Hyderabad 500078, Andhra Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 11期

关键词：

2-Chloronicotinaldehydes; 1H-1,2,3-Triazolylbenzohydrazides; Click chemistry; Anti-mycobacterial activity; Cytotoxicity; MYCOBACTERIUM-TUBERCULOSIS; POTENTIAL ANTIMYCOBACTERIAL; ANTITUBERCULOSIS ACTIVITY; ANTICANCER AGENTS; CLICK CHEMISTRY; DERIVATIVES; HYDRAZONES; INHIBITORS; GROWTH; DESIGN;

D O I：

10.1016/j.bmcl.2015.04.009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

1H-1,2,3-Triazolylbenzohydrazides (6a-h and 11a-l) were synthesized from 2-chloronicotinaldehydes and evaluated for anti-mycobacterial activity against Mycobacterium tuberculosis H(37)Rv strain (ATCC-27294). Seven compounds 6b, 6e, f, 11d, 11h, 11j and 11l displayed potent anti-mycobacterial activity (MIC 2.8-6.2 mu M). Potent anti-mycobacterial compounds were chosen for cytotoxicity studies by MTT protein assay against normal cell lines (PBMC and Raw 264.7) and shown low cytotoxicity. This is the first Letter assigning anti-mycobacterial activity, cytotoxicity and structure activity relationship for 1H-1,2, 3-triazolylbenzohydrazides. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：2390 / 2394

页数：5

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