1375313-78-2Relevant articles and documents
An efficient synthesis of 3-triazolyl-2(1H)-quinolones by CuTC-catalyzed azide-alkyne cycloaddition reaction
Messaoudi, Samir,Gabillet, Marie,Brion, Jean-Daniel,Alami, Mouad
, p. 155 - 158 (2013/04/24)
A facile and efficient Cu(I)-catalyzed azide-alkyne cycloaddition reaction for the synthesis of a series of 3-triazolyl-2(1H)-quinolones 3 have been developed using 3-azido-quinolin-2(1H)-one as the coupling partner. The optimized reaction conditions involve the use of eco- friendly ethanol as the solvent in the presence of copper(I) thiophene-2-carboxylate as the catalyst, to afford good to excellent yields of 3-triazolyl-2(1H)-quinolone derivatives of biological interest. Copyright
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
experimental part, p. 44 - 50 (2012/07/16)
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.