title: Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease.
abstract: The first series of peptidyl aldehyde inhibitors that incorporate in their structure a glutamine surrogate has been designed and synthesized based on the known substrate specificity of Norwalk virus 3C protease. The inhibitory activity of the compounds with the protease and with a norovirus cell-based replicon system was investigated. Members of this class of compounds exhibited noteworthy activity both in vitro and in a cell-based replicon system.
authors.affiliation: Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
authors.forename: Kok-Chuan
authors.initials: KC
authors.lastname: Tiew
authors.forename: Guijia
authors.initials: G
authors.lastname: He
authors.forename: Sridhar
authors.initials: S
authors.lastname: Aravapalli
authors.forename: Sivakoteswara Rao
authors.initials: SR
authors.lastname: Mandadapu
authors.forename: Mallikarjuna Reddy
authors.initials: MR
authors.lastname: Gunnam
authors.forename: Kevin R
authors.initials: KR
authors.lastname: Alliston
authors.forename: Gerald H
authors.initials: GH
authors.lastname: Lushington
authors.forename: Yunjeong
authors.initials: Y
authors.lastname: Kim
authors.forename: Kyeong-Ok
authors.initials: KO
authors.lastname: Chang
authors.forename: William C
authors.initials: WC
authors.lastname: Groutas
mesh_terms: D060326:Chemistry Techniques, Synthetic; D018360:Crystallography, X-Ray; D057056:Cysteine Proteases / Q000378:metabolism*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D008958:Models, Molecular; D008968:Molecular Conformation; D009663:Norwalk virus / Q000201:enzymology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D015853:Cysteine Proteinase Inhibitors; D057056:Cysteine Proteases