Discovery of new thienopyrimidinone derivatives displaying antimalarial properties toward both erythrocytic and hepatic stages of Plasmodium

…, MD Crozet, P Rathelot, P Dallemagne…

Index: Cohen, Anita; Crozet, Maxime D.; Rathelot, Pascal; Azas, Nadine; Vanelle, Patrice Molecules, 2013 , vol. 18, # 1 p. 97 - 113

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Citation Number: 5

Abstract

Abstract A preliminary in vitro screening of compounds belonging to various chemical families from our library revealed the thieno [3, 2-d] pyrimidin-4 (3H)-one scaffold displayed a promising profile against Plasmodium falciparum. Then, 120 new derivatives were synthesized and evaluated in vitro; compared to drug references, 40 showed good activity toward chloroquine sensitive (IC 50 35–344 nM) and resistant (IC 50 45–800 nM) P. ...