title: Synthesis and biological activity of peptidyl aldehyde urokinase inhibitors.
abstract: Solid- and solution-phase synthesis of peptidomimetic inhibitors of urokinase-type plasminogen activator based on the sequence dSerAlaArg-al are described. The biological activities of these unique inhibitors are reported herein. Carbonate prodrugs were prepared and tested as potential drug delivery systems.
authors.affiliation: Corvas International, Inc., Department of Medicinal Chemistry, San Diego, CA 92121, USA.
authors.forename: S Y
authors.initials: SY
authors.lastname: Tamura
authors.forename: M I
authors.initials: MI
authors.lastname: Weinhouse
authors.forename: C A
authors.initials: CA
authors.lastname: Roberts
authors.forename: E A
authors.initials: EA
authors.lastname: Goldman
authors.forename: K
authors.initials: K
authors.lastname: Masukawa
authors.forename: S M
authors.initials: SM
authors.lastname: Anderson
authors.forename: C R
authors.initials: CR
authors.lastname: Cohen
authors.forename: A E
authors.initials: AE
authors.lastname: Bradbury
authors.forename: V T
authors.initials: VT
authors.lastname: Bernardino
authors.forename: S A
authors.initials: SA
authors.lastname: Dixon
authors.forename: M G
authors.initials: MG
authors.lastname: Ma
authors.forename: T G
authors.initials: TG
authors.lastname: Nolan
authors.forename: T K
authors.initials: TK
authors.lastname: Brunck
mesh_terms: D000447:Aldehydes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D019540:Area Under Curve; D002851:Chromatography, High Pressure Liquid; D004151:Dipeptides / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006207:Half-Life; D011355:Prodrugs / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D010959:Tissue Plasminogen Activator / Q000037:antagonists & inhibitors; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*
chemical_list: D000447:Aldehydes; D004151:Dipeptides; D004791:Enzyme Inhibitors; D011355:Prodrugs; D010959:Tissue Plasminogen Activator; D005341:Fibrinolysin; D014568:Urokinase-Type Plasminogen Activator