Synthesis and in vitro anti-tubercular evaluation of 1,2,3-triazole tethered β-lactam-ferrocene and β-lactam-ferrocenylchalcone chimeric scaffolds

被引：52

作者：

Kumar, Kewal ^{[1
]}

Singh, Pardeep ^{[1
]}

Kremer, Laurent ^{[2
,3
]}

Guerardel, Yann ^{[4
,5
]}

Biot, Christophe ^{[4
,5
]}

Kumar, Vipan ^{[1
]}

机构：

[1] Guru Nanak Dev Univ, Dept Chem, Amritsar 143005, Punjab, India

[2] Univ Montpellier II & I, Lab Dynam Interact Membranaires Normales & Pathol, CNRS, UMR 5235, F-34095 Montpellier 05, France

[3] INSERM, DIMNP, F-34095 Montpellier 05, France

[4] Univ Lille 1, Univ Lille Nord France, Unite Glycobiol Struct & Fonct, F-59650 Villeneuve Dascq, France

[5] CNRS, UMR 8576, F-59650 Villeneuve Dascq, France

来源：

DALTON TRANSACTIONS | 2012年 / 41卷 / 19期

关键词：

RESISTANCE; CHALCONES;

D O I：

10.1039/c2dt30514c

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Twenty different triazoles were prepared to probe the antitubercular structure-activity relationships (SAR) within the beta-lactam-ferrocene-triazole conjugate family. The compounds have been synthesized by copper-catalyzed "click chemistry". In vitro anti-tubercular activity was determined for each compound but the synthesized hybrids failed to inhibit Mycobacterium tuberculosis growth even at high doses. The manuscript assumes significance as this is the first report on the inclusion of ferrocene nucleus in the well established beta-lactam family via triazole linkers with reputed physicochemical profiles.

引用

页码：5778 / 5781

页数：4

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