title: Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
abstract: A series of dipeptide nitriles with a thienyl alanine in P2 were identified as potent and selective cathepsin C inhibitors. Incorporation of a substituted cyclopropyl moiety in P1 effectively protects these derivatives against hydrolase activity in whole blood.
authors: Department of Medicinal Chemistry, Merck Frosst Canada & Co., 16711 Trans Canada Hwy, Kirkland, QC, Canada H9H 3L1.
authors: Daniel
authors: D
authors: Guay
authors: Christian
authors: C
authors: Beaulieu
authors: Jean-Francois
authors: JF
authors: Truchon
authors: T
authors: T
authors: Jagadeeswar Reddy
authors: Robert
authors: R
authors: Zamboni
authors: Christopher I
authors: CI
authors: Bayly
authors: Nathalie
authors: N
authors: Methot
authors: Joel
authors: J
authors: Rubin
authors: Diane
authors: D
authors: Ethier
authors: M
authors: M
authors: David Percival
mesh_terms: D000818:Animals; D020789:Cathepsin C / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D002460:Cell Line; D004151:Dipeptides / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D009570:Nitriles / Q000097:blood / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D004151:Dipeptides; D009570:Nitriles; D020789:Cathepsin C