Matches in SemOpenAlex for { <https://semopenalex.org/work/W2083762132> ?p ?o ?g. }
- W2083762132 endingPage "160" @default.
- W2083762132 startingPage "154" @default.
- W2083762132 abstract "ABSTRACT The Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3 appear to be required for hemoglobin hydrolysis by intraerythrocytic malaria parasites. Previous studies showed that peptidyl vinyl sulfone inhibitors of falcipain-2 blocked the development of P. falciparum in culture and exerted antimalarial effects in vivo. We now report the structure-activity relationships for inhibition of falcipain-2, falcipain-3, and parasite development by 39 new vinyl sulfone, vinyl sulfonate ester, and vinyl sulfonamide cysteine protease inhibitors. Levels of inhibition of falcipain-2 and falcipain-3 were generally similar, and many potent compounds were identified. Optimal antimalarial compounds, which inhibited P. falciparum development at low nanomolar concentrations, were phenyl vinyl sulfones, vinyl sulfonate esters, and vinyl sulfonamides with P 2 leucine moieties. Our results identify independent structural correlates of falcipain inhibition and antiparasitic activity and suggest that peptidyl vinyl sulfones have promise as antimalarial agents." @default.
- W2083762132 created "2016-06-24" @default.
- W2083762132 creator A5006216717 @default.
- W2083762132 creator A5045681846 @default.
- W2083762132 creator A5048049612 @default.
- W2083762132 creator A5055521023 @default.
- W2083762132 creator A5060280816 @default.
- W2083762132 creator A5064057534 @default.
- W2083762132 creator A5071690475 @default.
- W2083762132 creator A5077631479 @default.
- W2083762132 date "2003-01-01" @default.
- W2083762132 modified "2023-10-16" @default.
- W2083762132 title "Structure-Activity Relationships for Inhibition of Cysteine Protease Activity and Development of <i>Plasmodium falciparum</i> by Peptidyl Vinyl Sulfones" @default.
- W2083762132 cites W1967298004 @default.
- W2083762132 cites W1974021739 @default.
- W2083762132 cites W1976757612 @default.
- W2083762132 cites W1979446384 @default.
- W2083762132 cites W1989792394 @default.
- W2083762132 cites W2002816714 @default.
- W2083762132 cites W2008590973 @default.
- W2083762132 cites W2009972285 @default.
- W2083762132 cites W2016846877 @default.
- W2083762132 cites W2020251171 @default.
- W2083762132 cites W2024771347 @default.
- W2083762132 cites W2029985793 @default.
- W2083762132 cites W2034362842 @default.
- W2083762132 cites W2040912042 @default.
- W2083762132 cites W2046530591 @default.
- W2083762132 cites W2055813456 @default.
- W2083762132 cites W2057331899 @default.
- W2083762132 cites W2060825760 @default.
- W2083762132 cites W2070369762 @default.
- W2083762132 cites W2081327421 @default.
- W2083762132 cites W2084064912 @default.
- W2083762132 cites W2084466907 @default.
- W2083762132 cites W2087019614 @default.
- W2083762132 cites W2103700658 @default.
- W2083762132 cites W2106220465 @default.
- W2083762132 cites W2112941164 @default.
- W2083762132 cites W2127137755 @default.
- W2083762132 cites W2128378359 @default.
- W2083762132 cites W2131316262 @default.
- W2083762132 cites W2145951150 @default.
- W2083762132 cites W2152921443 @default.
- W2083762132 cites W2160649586 @default.
- W2083762132 cites W2162324851 @default.
- W2083762132 cites W2165174924 @default.
- W2083762132 cites W2169149151 @default.
- W2083762132 cites W2176557328 @default.
- W2083762132 cites W2326613008 @default.
- W2083762132 cites W2950364520 @default.
- W2083762132 cites W2951217290 @default.
- W2083762132 cites W4248713218 @default.
- W2083762132 doi "https://doi.org/10.1128/aac.47.1.154-160.2003" @default.
- W2083762132 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/149004" @default.
- W2083762132 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12499184" @default.
- W2083762132 hasPublicationYear "2003" @default.
- W2083762132 type Work @default.
- W2083762132 sameAs 2083762132 @default.
- W2083762132 citedByCount "150" @default.
- W2083762132 countsByYear W20837621322012 @default.
- W2083762132 countsByYear W20837621322013 @default.
- W2083762132 countsByYear W20837621322014 @default.
- W2083762132 countsByYear W20837621322015 @default.
- W2083762132 countsByYear W20837621322016 @default.
- W2083762132 countsByYear W20837621322017 @default.
- W2083762132 countsByYear W20837621322018 @default.
- W2083762132 countsByYear W20837621322019 @default.
- W2083762132 countsByYear W20837621322020 @default.
- W2083762132 countsByYear W20837621322021 @default.
- W2083762132 countsByYear W20837621322022 @default.
- W2083762132 countsByYear W20837621322023 @default.
- W2083762132 crossrefType "journal-article" @default.
- W2083762132 hasAuthorship W2083762132A5006216717 @default.
- W2083762132 hasAuthorship W2083762132A5045681846 @default.
- W2083762132 hasAuthorship W2083762132A5048049612 @default.
- W2083762132 hasAuthorship W2083762132A5055521023 @default.
- W2083762132 hasAuthorship W2083762132A5060280816 @default.
- W2083762132 hasAuthorship W2083762132A5064057534 @default.
- W2083762132 hasAuthorship W2083762132A5071690475 @default.
- W2083762132 hasAuthorship W2083762132A5077631479 @default.
- W2083762132 hasBestOaLocation W20837621322 @default.
- W2083762132 hasConcept C178790620 @default.
- W2083762132 hasConcept C181199279 @default.
- W2083762132 hasConcept C182220744 @default.
- W2083762132 hasConcept C185592680 @default.
- W2083762132 hasConcept C203014093 @default.
- W2083762132 hasConcept C2776714187 @default.
- W2083762132 hasConcept C2777283782 @default.
- W2083762132 hasConcept C2778048844 @default.
- W2083762132 hasConcept C2778371730 @default.
- W2083762132 hasConcept C2778806918 @default.
- W2083762132 hasConcept C2779201268 @default.
- W2083762132 hasConcept C2781039511 @default.
- W2083762132 hasConcept C55493867 @default.
- W2083762132 hasConcept C71240020 @default.
- W2083762132 hasConcept C86803240 @default.
- W2083762132 hasConceptScore W2083762132C178790620 @default.