1. Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
- Author
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Glória PM, Gut J, Gonçalves LM, Rosenthal PJ, Moreira R, and Santos MM
- Subjects
- Antimalarials chemical synthesis, Cysteine Endopeptidases metabolism, Erythrocytes parasitology, Humans, Inhibitory Concentration 50, Malaria, Falciparum drug therapy, Plasmodium falciparum enzymology, Sulfones chemical synthesis, Antimalarials chemistry, Antimalarials pharmacology, Plasmodium falciparum drug effects, Sulfones chemistry, Sulfones pharmacology
- Abstract
A series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents. Tested compounds did not show activity against papain or the Plasmodium falciparum cysteine protease falcipain-2. However, a number of the new compounds effectively inhibited the in vitro development of P. falciparum. Compounds containing a squaramide group were the most active, with IC(50) values between 0.95 and 4.5 μM, suggesting that these are potential lead compounds for the development of new antimalarial agents., (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Published
- 2011
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