title: Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
abstract: A series of pyrroloquinazolines has been discovered that represent novel small molecule inhibitors of the intramolecular ligand of the thrombin receptor. Analogs were prepared to study the structure-activity relationships of substitution at the N 1, N3, and N7 positions of the heterocycle. Compounds 4e and 4f have been identified with IC50's of 56 and 52 nM, respectively.
authors.affiliation: Schering-Plough Research Institute, Kenilworth, NJ 07033-0539, USA.
authors.forename: H S
authors.initials: HS
authors.lastname: Ahn
authors.forename: L
authors.initials: L
authors.lastname: Arik
authors.forename: G
authors.initials: G
authors.lastname: Boykow
authors.forename: D A
authors.initials: DA
authors.lastname: Burnett
authors.forename: M A
authors.initials: MA
authors.lastname: Caplen
authors.forename: M
authors.initials: M
authors.lastname: Czarniecki
authors.forename: M S
authors.initials: MS
authors.lastname: Domalski
authors.forename: C
authors.initials: C
authors.lastname: Foster
authors.forename: M
authors.initials: M
authors.lastname: Manna
authors.forename: A W
authors.initials: AW
authors.lastname: Stamford
authors.forename: Y
authors.initials: Y
authors.lastname: Wu
mesh_terms: D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D044463:Receptor, PAR-1; D018179:Receptors, Thrombin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000494:pharmacology
chemical_list: D010975:Platelet Aggregation Inhibitors; D011758:Pyrroles; D011799:Quinazolines; D044463:Receptor, PAR-1; D018179:Receptors, Thrombin; D013917:Thrombin