Pj. Rosenthal et al., ANTIMALARIAL EFFECTS OF VINYL SULFONE CYSTEINE PROTEINASE-INHIBITORS, Antimicrobial agents and chemotherapy, 40(7), 1996, pp. 1600-1603
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.