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

被引：28
|
作者：
Dubar, Faustine [1 ]
Wintjens, Rene [2 ]
Martins-Duarte, Erica S. [3 ]
Vommaro, Rossiane C. [3 ]
de Souza, Wanderley [3 ]
Dive, Daniel [4 ]
Pierrot, Christine [4 ]
Pradines, Bruno [5 ]
Wohlkonig, Alexandre [6 ]
Khalife, Jamal [4 ]
Biot, Christophe [1 ,7 ]
机构：
[1] Univ Lille 1, ENSCL, Unite Catalyse & Chim Solide, UMR 8181,CNRS,Univ Lille Nord France, F-59652 Villeneuve Dascq, France
[2] Univ Libre Bruxelles, Fac Pharm, Lab Chim Gen, B-1050 Brussels, Belgium
[3] Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, Lab Ultraestrutura Celular Hertha Meyer, BR-21941902 Rio De Janeiro, Brazil
[4] Univ Lille Nord France, Inst Pasteur Lille, INSERM, CIIL,U1019,UMR 8024,CNRS, F-59019 Lille, France
[5] Inst Rech Biomed Armees, Unite Parasitol, URMITE UMR 6236, F-13262 Marseille 07, France
[6] VIB, B-1050 Brussels, Belgium
[7] Univ Lille 1, Unite Glycobiol Struct & Fonct, CNRS, UMR 8576,IFR 147,Univ Lille Nord France, F-59650 Villeneuve Dascq, France
来源：
MEDCHEMCOMM | 2011年 / 2卷 / 05期
关键词：
PLASMODIUM-FALCIPARUM; ANTIBACTERIAL EVALUATION; ANTIBIOTICS; 6-AMINOQUINOLONES; FERROQUINE; TARGET;
D O I：
10.1039/c1md00022e
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
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.
引用
收藏
页码：430 / 435
页数：6
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