title: Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 2: design of potent antagonists containing the 3-azaspiro[5.5]undecanes.
abstract: The synthesis and biological activity of novel glycoprotein IIb-IlIa anatagonists containing 3-azaspiro[5.5]undec-9-yl nucleus are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the monoazaspirocyclic structure as central template for nonpeptide RGD mimics.
authors.affiliation: COR Therapeutics, Inc, Department of Medicinal Chemistry and Biology, South San Francisco, CA 94080, USA.
authors.forename: A
authors.initials: A
authors.lastname: Pandey
authors.forename: J
authors.initials: J
authors.lastname: Seroogy
authors.forename: D
authors.initials: D
authors.lastname: Volkots
authors.forename: M S
authors.initials: MS
authors.lastname: Smyth
authors.forename: J
authors.initials: J
authors.lastname: Rose
authors.forename: M M
authors.initials: MM
authors.lastname: Mehrotra
authors.forename: J
authors.initials: J
authors.lastname: Heath
authors.forename: G
authors.initials: G
authors.lastname: Ruhter
authors.forename: T
authors.initials: T
authors.lastname: Schotten
authors.forename: R M
authors.initials: RM
authors.lastname: Scarborough
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis / Q000493:pharmacokinetics / Q000494:pharmacology; D001682:Biological Availability; D001792:Blood Platelets / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D019039:Platelet Glycoprotein GPIIb-IIIa Complex / Q000037:antagonists & inhibitors*; D051381:Rats; D017207:Rats, Sprague-Dawley; D019030:Receptors, Vitronectin / Q000037:antagonists & inhibitors; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; D010975:Platelet Aggregation Inhibitors; D019039:Platelet Glycoprotein GPIIb-IIIa Complex; D019030:Receptors, Vitronectin; D013141:Spiro Compounds