Design, synthesis and structure–activity relationships of (1H-pyridin-4-ylidene) amines as potential antimalarials

…, M Carrasco, J Gut, PJ Rosenthal, R Moreira…

Index: Rodrigues, Tiago; Guedes, Rita C.; dos Santos, Daniel J.V.A.; Carrasco, Marta; Gut, Jiri; Rosenthal, Philip J.; Moreira, Rui; Lopes, Francisca Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 13 p. 3476 - 3480

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Citation Number: 16

Abstract

(1H-Pyridin-4-ylidene) amines containing lipophilic side chains at the imine nitrogen atom were prepared as potential clopidol isosteres in the development of antimalarials. Their antiplasmodial activity was evaluated in vitro against the Plasmodium falciparum W2 (chloroquine-resistant) and FCR3 (atovaquone-resistant) strains. The most active of these derivatives, 4m, had an IC50 of 1μM against W2 and 3μM against FCR3. Molecular ...