Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.
A simple and versatile method for preparation of (D)-Phe-Pro peptidomimetic bicyclic thiazolidine lactams is presented. These bicyclic lactams have chemical diversity alpha to the lactam carbonyl and, when linked to electrophilic arginines, provide potent thrombin inhibitors.
Bachand
B
B
BioChem Therapeutic Inc., Laval, Québec, Canada.
DiMaio
J
J
Siddiqui
M A
MA
D000991:Antithrombins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007769:Lactams / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000991:Antithrombins; D001643:Bridged Bicyclo Compounds; D007769:Lactams