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Title: Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials
Authors: Kumar, S. Praveen
Gut, Jiri
Guedes, Rita C.
Rosenthal, Philip J.
Santos, Maria M. M.
Moreira, Rui
Keywords: Indolin-2-ones
Falcipain inhibitor
Antiplasmodial activity
Issue Date: 2011
Publisher: Elsevier
Citation: Kumar, S. Praveen; Gut, Jiri; Guedes, Rita C. ; Rosenthal, Philip J.; Santos, Maria M. M.; Moreira, Rui. Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarials, European Journal of Medicinal Chemistry, 46, 927-933, 2011.
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 the related protease falcipain-3, and displayed antiplasmodial activity against the chloroquine-resistant P. falciparum W2 strain in the low micromolar range. Coupling a 7-chloroquinoline moiety to the 3-methylene-substituted indolinone scaffold led to a significant improvement in antiplasmodial activity.
Peer review: yes
ISSN: 0223-5234
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Appears in Collections:FF-DQFT - Artigos em Revistas Internacionais

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