title: Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain.
abstract: A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000s(-1)M(-1) versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.
authors.affiliation: Department of Chemistry, University of Michigan, Ann Arbor, 48109, USA. roush@umich.edu
authors.forename: W R
authors.initials: WR
authors.lastname: Roush
authors.forename: J
authors.initials: J
authors.lastname: Cheng
authors.forename: B
authors.initials: B
authors.lastname: Knapp-Reed
authors.forename: A
authors.initials: A
authors.lastname: Alvarez-Hernandez
authors.forename: J H
authors.initials: JH
authors.lastname: McKerrow
authors.forename: E
authors.initials: E
authors.lastname: Hansell
authors.forename: J C
authors.initials: JC
authors.lastname: Engel
mesh_terms: D000818:Animals; D003546:Cysteine Endopeptidases / Q000378:metabolism; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D021261:Parasitic Sensitivity Tests; D015800:Protozoan Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014349:Trypanosoma cruzi / Q000187:drug effects*
chemical_list: D015853:Cysteine Proteinase Inhibitors; D015800:Protozoan Proteins; D013449:Sulfonamides; D014344:Trypanocidal Agents; C440389:vinyl sulfonamide; D003546:Cysteine Endopeptidases; C074032:cruzain, Trypanosoma cruzi