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

Faustine Dubar (1) , René Wintjens (2) , E. S. Martins-Duarte (3) , R. C. Vommaro (3) , W. de Souza (3) , Daniel Dive (4) , C. Pierrot (5) , Bruno Pradines (6) , A. Wohlkönig (7) , Jamal Khalife (4) , Christophe Biot (1, 8)

1 UCCS - Unité de Catalyse et Chimie du Solide - UMR 8181
2 Laboratoire de Chimie Générale
3 Laboratório de Ultraestrutura Celular Hertha Meyer - IBCCF / UFRJ [Rio de Janeiro]
4 Schistosomiase, paludisme et inflammation
5 CIIL - Centre d’Infection et d’Immunité de Lille - INSERM U 1019 - UMR 9017 - UMR 8204
6 Unité de Recherche en Biologie et Epidémiologie Parasitaires
7 Structural Biology Brussels and Molecular and Cellular Interactions
8 UGSF - Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576

Novel ester prodrugs 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.

Domaines: Biochimie [q-bio.BM]

Faustine Dubar, René Wintjens, E. S. Martins-Duarte, R. C. Vommaro, W. de Souza, et al.. Ester prodrugs of ciprofloxacin as DNA-gyrase inhibitors: Synthesis, antiparasitic evaluation and docking studies. MedChemComm, 2011, 2 (5), pp.430-435. ⟨10.1039/c1md00022e⟩. ⟨hal-00641730⟩