Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

D Audisio, S Messaoudi, S Cojean, JF Peyrat…

Index: Audisio, Davide; Messaoudi, Samir; Cojean, Sandrine; Peyrat, Jean-Francois; Brion, Jean-Daniel; Bories, Christian; Huteau, Francoise; Loiseau, Philippe M.; Alami, Mouad European Journal of Medicinal Chemistry, 2012 , vol. 52, p. 44 - 50

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Citation Number: 15

Abstract

A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure–activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC50 values in a range of 2–11 μM). Additionally, compound ...