ANTIMALARIAL EFFECTS OF VINYL SULFONE CYSTEINE PROTEINASE-INHIBITORS

Citation
Pj. Rosenthal et al., ANTIMALARIAL EFFECTS OF VINYL SULFONE CYSTEINE PROTEINASE-INHIBITORS, Antimicrobial agents and chemotherapy, 40(7), 1996, pp. 1600-1603
Citations number
18
Categorie Soggetti
Pharmacology & Pharmacy",Microbiology
ISSN journal
00664804
Volume
40
Issue
7
Year of publication
1996
Pages
1600 - 1603
Database
ISI
SICI code
0066-4804(1996)40:7<1600:AEOVSC>2.0.ZU;2-K
Abstract
We evaluated the antimalarial effects of vinyl sulfone cysteine protei nase inhibitors, A number of vinyl sulfones strongly inhibited falcipa in, a Plasmodium falciparum cysteine proteinase that is a critical hem oglobinase. In studies of cultured parasites, nanomolar concentrations of three vinyl sulfones inhibited parasite hemoglobin degradation, me tabolic activity, and development, The antimalarial effects correlated with the inhibition of falcipain, Our results suggest that vinyl sulf ones or related cysteine proteinase inhibitors may have promise as ant imalarial agents.