title: Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes.
abstract: The synthesis and biological activity of analogues containing spiro piperidinylpyridine and pyrrolidinylpyridine templates are described. The potent activity of these compounds as platelet aggregation inhibitors demonstrates the utility of the spiro structures as central template for nonpeptide RGD mimics.
authors.affiliation: COR Therapeutics, Inc., Department of Medicinal Chemistry, South San Francisco, CA 94080, USA.
authors.forename: Mukund M
authors.initials: MM
authors.lastname: Mehrotra
authors.forename: Julie A
authors.initials: JA
authors.lastname: Heath
authors.forename: Jack W
authors.initials: JW
authors.lastname: Rose
authors.forename: Mark S
authors.initials: MS
authors.lastname: Smyth
authors.forename: Joseph
authors.initials: J
authors.lastname: Seroogy
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Volkots
authors.forename: Gerd
authors.initials: G
authors.lastname: Ruhter
authors.forename: Theo
authors.initials: T
authors.lastname: Schotten
authors.forename: Lisa
authors.initials: L
authors.lastname: Alaimo
authors.forename: Gary
authors.initials: G
authors.lastname: Park
authors.forename: Anjali
authors.initials: A
authors.lastname: Pandey
authors.forename: Robert 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; 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; D013141:Spiro Compounds