Issue 11, 2011
From the journal:

New Journal of Chemistry

One-pot microwave-assisted synthesis and antimalarial activity of ferrocenylbenzodiazepines†

Gabin Mwande-Maguene,a   Jouda Jakhlal,a   Jean-Bernard Lekana-Douki,b   Elisabeth Mouray,c   Till Bousquet,a   Sylvain Pellegrini,a   Philippe Grellier,c   Fousseyni Samba Toure Ndouo,b   Jacques Lebibi*d  and  Lydie Pelinski*a  

* Corresponding authors

a Université Lille Nord de France, Université de Lille1, Unité de Catalyse et de Chimie du Solide, CNRS UMR 8181, ENSCL, 59652 Villeneuve d'Ascq, France
E-mail: lydie.pelinski@ensc-lille.fr

b Centre International de Recherches Médicales de Franceville (CIRMF), Unité de Parasitologie, BP 769 Franceville, Gabon

c FRE 3206 CNRS MCAM, Muséum National d'Histoire Naturelle, Département Régulations, Développement, Diversité Moléculaire CP 52, 61 rue Buffon, 75231 Paris Cedex 05, France

d Université des Sciences et Techniques de Masuku, BP 901, Franceville, Gabon
E-mail: jlebibi@hotmail.com

Abstract

An efficient synthesis of 1,4-benzodiazepin-2-ones is described by condensation between 2-aminobenzophenone and Boc-protected amino acids via microwave-assisted irradiation. This produces higher yields in shorter reaction times than with traditional methods. The antiplasmodial activity of the corresponding ferrocenyl benzodiazepines was evaluated in vitro against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquine-resistant) strains and gabonese clinical isolates.

Graphical abstract: One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines

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Article information

DOI
https://doi.org/10.1039/C1NJ20551J
Article type
Letter
Submitted
22 Jun 2011
Accepted
30 Aug 2011
First published
28 Sep 2011

New J. Chem., 2011,35, 2412-2415

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One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines

G. Mwande-Maguene, J. Jakhlal, J. Lekana-Douki, E. Mouray, T. Bousquet, S. Pellegrini, P. Grellier, F. S. T. Ndouo, J. Lebibi and L. Pelinski, New J. Chem., 2011, 35, 2412 DOI: 10.1039/C1NJ20551J

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