Synthesis and In Vitro Antibacterial Evaluation of Mannich Base Nitrothiazole Derivatives

被引：2

作者：

Dube, Phelelisiwe S. ^{[1
]}

Hart, Dylan ^{[1
]}

Legoabe, Lesetja J. ^{[1
]}

Jordaan, Audrey ^{[2
]}

Warner, Digby F. ^{[2
,3
,4
]}

Beteck, Richard M. ^{[1
]}

机构：

[1] North West Univ, Ctr Excellence Pharmaceut Sci, ZA-2520 Potchefstroom, South Africa

[2] Univ Cape Town, Dept Pathol, SAMRC NHLS UCT Mol Mycobacteriol Res Unit, ZA-7925 Observatory, South Africa

[3] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa

[4] Univ Cape Town, Fac Hlth Sci, Welcome Ctr Infect Dis Res Africa CIDRI Africa, ZA-7701 Rondebosch, South Africa

来源：

MOLBANK | 2024年 / 2024卷 / 01期

基金：

英国医学研究理事会; 英国惠康基金; 新加坡国家研究基金会;

关键词：

nitrothiazole; Mannich bases; antitubercular activity; tuberculosis; Mycobacterium tuberculosis; MYCOBACTERIUM-TUBERCULOSIS;

D O I：

10.3390/M1793

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Nitrothiazole derivatives have been reported to exhibit activity against aerobic, anaerobic, and microaerophilic bacteria. This activity profile makes the nitrothiazole compound class an ideal lead source against Mycobacterium tuberculosis, which flourishes in varied environments with different oxygen concentrations. In this work, we investigated six nitrothiazole derivatives for antitubercular activity. The compounds exhibited potent activity, with compounds 9 and 10 possessing an equipotent MIC90 value of 0.24 mu M. The compounds were investigated for cytotoxicity against HEK293 cells and hemolysis against red blood cells, and they demonstrated no cytotoxicity nor hemolytic effects, suggesting they possess inherent antitubercular activity.

引用

页数：8

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