title: Potent bicyclic lactam inhibitors of thrombin: Part I: P3 modifications.
abstract: Peptidomimetic inhibitors of general structure 1 have been prepared. Optimization of the binding affinities of these compounds through variation of the P3 hydrophobic residue is described. Selected substituted bicylic lactams displayed interesting pharmacological profiles both in vitro and in vivo.
authors.affiliation: BioChem Therapeutic Inc., Laval, Québec, Canada.
authors.forename: Y
authors.initials: Y
authors.lastname: St-Denis
authors.forename: C E
authors.initials: CE
authors.lastname: Augelli-Szafran
authors.forename: B
authors.initials: B
authors.lastname: Bachand
authors.forename: K A
authors.initials: KA
authors.lastname: Berryman
authors.forename: J
authors.initials: J
authors.lastname: DiMaio
authors.forename: A M
authors.initials: AM
authors.lastname: Doherty
authors.forename: J J
authors.initials: JJ
authors.lastname: Edmunds
authors.forename: L
authors.initials: L
authors.lastname: Leblond
authors.forename: S
authors.initials: S
authors.lastname: Lévesque
authors.forename: L S
authors.initials: LS
authors.lastname: Narasimhan
authors.forename: J R
authors.initials: JR
authors.lastname: Penvose-Yi
authors.forename: J R
authors.initials: JR
authors.lastname: Rubin
authors.forename: M
authors.initials: M
authors.lastname: Tarazi
authors.forename: P D
authors.initials: PD
authors.lastname: Winocour
authors.forename: M A
authors.initials: MA
authors.lastname: Siddiqui
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007769:Lactams / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000037:antagonists & inhibitors*
chemical_list: D005343:Fibrinolytic Agents; D007769:Lactams; D015842:Serine Proteinase Inhibitors; D013917:Thrombin