Browsing by Author "Kumar, S. Praveen"
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- Design and synthesis 3-methylene indolinones as antimalarialsPublication . Kumar, S. Praveen; Santos, Maria M. M.; Moreira, Rui
- Design, synthesis and evaluation of 3-methylene-substituted indolinones as antimalarialsPublication . Kumar, S. Praveen; Gut, Jiri; Guedes, Rita C.; Rosenthal, Philip J.; Santos, Maria M. M.; Moreira, RuiThe 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.
- Efficient synthesis of spiroisoxazoline oxindolesPublication . Ribeiro, Carlos J. A.; Kumar, S. Praveen; Moreira, Rui; Santos, Maria M. M.The synthesis of spiroisoxazoline oxindoles containing ester groups at position 4′ and aromatic or ester groups at position 3′ of the isoxazoline ring is reported. The compounds were synthesized in yields up to 94% by 1,3-dipolar cycloaddition of 3-methylene indolin-2-ones and chlorooximes in the presence of triethylamine or zinc.
- Squaric acid: a valuable scaffold for developing antimalarials?Publication . Kumar, S. Praveen; Glória, Paulo M. C.; Gonçalves, Lídia M.; Gut, Jiri; Rosenthal, Philip J.; Moreira, Rui; Santos, Maria M. M.We describe here the synthesis of a library of thirty-eight squaric derivatives and the evaluation of activity against papain-, falcipain-2- and a chloroquine-resistant strain of P. falciparum. The most active compounds combine significant antiplasmodial activity with minimal cytotoxicity.
- Synthesis and anti-plasmodial evaluation of a library of squaramide derivativesPublication . Kumar, S. Praveen; Gut, Jiri; Rosenthal, Philip J.; Moreira, Rui; Santos, Maria M. M.