Convergent synthesis and biological evaluation of 3[2-(benzylidenehydrazinyl]thiazol-4-yl]-4-hydroxycoumarins

被引：1

作者：

Manyeruke, Meloddy H. ^{[1
]}

Tshiwawa, Tendamudzimu ^{[1
]}

Hoppe, Heinrich C. ^{[2
,3
]}

Isaacs, Michelle ^{[3
]}

Seldon, Ronnett ^{[4
]}

Warner, Digby F. ^{[5
,6
]}

Krause, Rui W. M. ^{[1
,3
]}

Kaye, Perry T. ^{[1
,3
]}

机构：

[1] Rhodes Univ, Dept Chem, ZA-6140 Makhanda Grahamstown, South Africa

[2] Rhodes Univ, Dept Biochem & Microbiol, ZA-6140 Makhanda Grahamstown, South Africa

[3] Rhodes Univ, Ctr Chem & Biomed Res CCBR, ZA-6140 Makhanda Grahamstown, South Africa

[4] Univ Cape Town, Drug Discovery & Dev Ctr H3 D, Dept Chem, ZA-7701 Rondebosch, South Africa

[5] Univ Cape Town, Dept Pathol, Mol Mycobacteriol Res Unit, Cape Town, South Africa

[6] Univ Cape Town, Inst Infect Dis & Mol Med, Cape Town, South Africa

来源：

ARKIVOC | 2022年

基金：

英国医学研究理事会;

关键词：

4-Hydroxycoumarin; thiazole; benzylidenehydrazine; synthesis; biological studies; ACTION HIV-1 PROTEASE; COUMARIN DERIVATIVES; NATURAL-PRODUCTS; DRUG; INTEGRASE;

D O I：

10.24820/ark.5550190.p011.725

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A convenient synthesis of a small library of 4-hydroxycoumarin derivatives, containing thiazole and benzylidenehydrazine moieties has been achieved, using 2-hydroxyacetophenone and aryl- and heteroaryl aldehydes as starting materials. In vitro biological studies revealed that some of the compounds exhibited modest activities, viz.; anti-malarial (65% PLDH viability), anti-trypanosomal (52% T.b.brucei viability), anti-mycobacterial (Visual MIC90 5.63 mu M) and anti-bacterial (restricting S.aureus metabolic activity after 6 h). [GRAPHICS] .

引用

页码：159 / 166

页数：8

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