Issue 19, 2012
From the journal:

Dalton Transactions

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

Kewal Kumar,a   Pardeep Singh,a   Laurent Kremer,bc   Yann Guérardel,de   Christophe Biotde  and  Vipan Kumar*a  

* Corresponding authors

a Department of Chemistry, Guru Nanak Dev University, Amritsar-143005, Punjab, India
E-mail: vipan_org@yahoo.com
Fax: +91-183-2258819-20
Tel: +91-183-2258802 extn. 3320

b Laboratoire de Dynamique des Interactions Membranaires Normales et Pathologiques, UMR 5235 CNRS, Université de Montpellier II et I, Place Eugène Bataillon, 34095 Montpellier Cedex 05, France

c INSERM, DIMNP, Place Eugène Bataillon, 34095 Montpellier Cedex 05, France

d Université Lille Nord de France, Université de Lille 1, Unité de Glycobiologie Structurale et Fonctionnelle, F-59650 Villeneuve d'Ascq, France

e CNRS, UMR 8576, F-59650 Villeneuve d'Ascq, France

Abstract

Twenty different triazoles were prepared to probe the anti-tubercular structure–activity relationships (SAR) within the β-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 β-lactam family via triazole linkers with reputed physicochemical profiles.

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

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Article information

DOI
https://doi.org/10.1039/C2DT30514C
Article type
Communication
Submitted
03 Mar 2012
Accepted
21 Mar 2012
First published
03 Apr 2012

Dalton Trans., 2012,41, 5778-5781

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

K. Kumar, P. Singh, L. Kremer, Y. Guérardel, C. Biot and V. Kumar, Dalton Trans., 2012, 41, 5778 DOI: 10.1039/C2DT30514C

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