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Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2011 Dec 15; Vol. 19 (24), pp. 7635-42. Date of Electronic Publication: 2011 Oct 14. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 19
- Issue :
- 24
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 22071522
- Full Text :
- https://doi.org/10.1016/j.bmc.2011.10.018