Issue 5, 2011
From the journal:

MedChemComm

Esterprodrugs of ciprofloxacin as DNA-gyrase inhibitors: synthesis, antiparasitic evaluation and docking studies†

Faustine Dubar,a   René Wintjens,b   Érica S. Martins-Duarte,c   Rossiane C. Vommaro,c   Wanderley de Souza,c   Daniel Dive,d   Christine Pierrot,d   Bruno Pradines,e   Alexandre Wohlkonig,f   Jamal Khalife‡d  and  Christophe Biot‡*ag  

* Corresponding authors

a Université Lille Nord de France, Université de Lille1, Unité de Catalyse et Chimie du Solide - UMR CNRS 8181, ENSCL, Bâtiment C7, B.P. 90108, Villeneuve d'Ascq Cedex, France

b Laboratoire de Chimie Générale, Facultés de Pharmacie, Université Libre de Bruxelles (ULB), Campus Plaine (CP 206/4), boulevard du Triomphe, Brussels, Belgium

c Laboratório de Ultraestrutura Celular Hertha Meyer, Instituto de Biofísica Carlos Chagas Filho, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil

d CIIL, Inserm U 1019, UMR CNRS 8024 Université Lille Nord de France, Institut Pasteur de Lille, 1 rue du Pr Calmette, Lille Cedex, France

e Institut de Recherche Biomédicale des Armées, Antenne de Marseille, Unité de Parasitologie, URMITE-UMR 6236, Allée du Médecin Colonel Jamot, Parc le Pharo, BP 60109, Marseille Cedex 07, France

f Structural Biology Brussels & Molecular and Cellular Interactions, VIB, Pleinlaan 2, Brussels, Belgium

g Université Lille Nord de France, Université de Lille1, Unité de Glycobiologie Structurale et Fonctionnelle, CNRS UMR 8576, IFR 147, Villeneuve d'Ascq Cédex, France
E-mail: christophe.biot@univ-lille1.fr
Fax: +33 320436555
Tel: +33 320436941

Abstract

Novel esterprodrugs of ciprofloxacin were synthesized, and tested for their antimalarial and antitoxoplasma activity. These new compounds proved to be extremely efficient against these parasites. Molecular modeling and computational calculations were used to understand the mechanisms of action of these drugs.

Graphical abstract: Ester prodrugs of ciprofloxacin as DNA-gyrase inhibitors: synthesis, antiparasitic evaluation and docking studies

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Article information

DOI
https://doi.org/10.1039/C1MD00022E
Article type
Concise Article
Submitted
20 Jan 2011
Accepted
03 Mar 2011
First published
17 Mar 2011

Med. Chem. Commun., 2011,2, 430-435

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Ester prodrugs of ciprofloxacin as DNA-gyrase inhibitors: synthesis, antiparasitic evaluation and docking studies

F. Dubar, R. Wintjens, É. S. Martins-Duarte, R. C. Vommaro, W. de Souza, D. Dive, C. Pierrot, B. Pradines, A. Wohlkonig, J. Khalife and C. Biot, Med. Chem. Commun., 2011, 2, 430 DOI: 10.1039/C1MD00022E

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