Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials

SP Kumar, J Gut, RC Guedes, PJ Rosenthal…

Index: Praveen Kumar; Gut, Jiri; Guedes, Rita C.; Rosenthal, Philip J.; Santos, Maria M.M.; Moreira, Rui European Journal of Medicinal Chemistry, 2011 , vol. 46, # 3 p. 927 - 933

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Citation Number: 18

Abstract

The design, synthesis and evaluation of 3-methylene-substituted indolinones as falcipain inhibitors and antiplasmodial agents are described. These compounds react readily with thiols via an addition-elimination mechanism, indicating their potential as cysteine protease inhibitors. Several indolinones containing a Leu-i-amyl recognition moiety were found to be moderate inhibitors of the Plasmodium falciparum cysteine protease falcipain-2, but not of ...