Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors-Reference-Cited by-同舟云学术

Antimalarial effects of vinyl sulfone cysteine proteinase inhibitors

Published:1996-07 Issue:7 Volume:40 Page:1600-1603
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Rosenthal P J¹,Olson J E¹,Lee G K¹,Palmer J T¹,Klaus J L¹,Rasnick D¹

Affiliation:

1. Department of Medicine, San Francisco General Hospital, University of California 94143, USA. rosnthl@itsa.ucsf.edu

Abstract

We evaluated the antimalarial effects of vinyl sulfone cysteine proteinase inhibitors. A number of vinyl sulfones strongly inhibited falcipain, a Plasmodium falciparum cysteine proteinase that is a critical hemoglobinase. In studies of cultured parasites, nanomolar concentrations of three vinyl sulfones inhibited parasite hemoglobin degradation, metabolic activity, and development. The antimalarial effects correlated with the inhibition of falcipain. Our results suggest that vinyl sulfones or related cysteine proteinase inhibitors may have promise as antimalarial agents.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.40.7.1600

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