1375313-79-3Relevant academic research and scientific papers
Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives
Audisio, Davide,Messaoudi, Samir,Cojean, Sandrine,Peyrat, Jean-Fran?ois,Brion, Jean-Daniel,Bories, Christian,Huteau, Fran?oise,Loiseau, Philippe M.,Alami, Mouad
, p. 44 - 50 (2012)
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.
