title: Synthesis of potent and selective inhibitors of human plasma kallikrein.
abstract: The synthesis and in vitro enzyme inhibition profile of a series of novel trifluoromethylketone (TFMK) inhibitors of human plasma kallikrein (PK) are described. We have developed an efficient method for the construction of peptide TFMKs that provides the final product devoid of compromised stereochemical integrity. Many of these compounds are potent inhibitors of PK and exhibit reduced inhibition of tissue kallikrein (TK) and plasmin (HP).
authors: Corporate Research Division, Miami Valley Laboratories, The Procter & Gamble Company, Cincinnati, OH 45253-8707, USA.
authors: G S
authors: GS
authors: Garrett
authors: S J
authors: SJ
authors: McPhail
authors: K
authors: K
authors: Tornheim
authors: P E
authors: PE
authors: Correa
authors: J M
authors: JM
authors: McIver
mesh_terms: D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006801:Humans; D007610:Kallikreins / Q000037:antagonists & inhibitors*; D007659:Ketones / Q000138:chemical synthesis* / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D007659:Ketones; D015842:Serine Proteinase Inhibitors; D007610:Kallikreins; D005341:Fibrinolysin