Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives.

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 (IC 50 values in a range of 2–11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T . b . brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.