title: Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
abstract: In our continuing efforts to identify small molecule vitronectin receptor antagonists, we have discovered a series of phenylbutyrate derivatives, exemplified by 16, which have good potency and excellent oral bioavailability (approximately 100% in rats). This new series is derived conceptually from opening of the seven-membered ring of SB-265123.
authors.affiliation: GlaxoSmithKline Pharmaceuticals, 1250 S. Collegeville Rd., PO Box 5089, PA 19426, USA. william_h_miller@gsk.com
authors.forename: William H
authors.initials: WH
authors.lastname: Miller
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Manley
authors.forename: Russell D
authors.initials: RD
authors.lastname: Cousins
authors.forename: Karl F
authors.initials: KF
authors.lastname: Erhard
authors.forename: Dirk A
authors.initials: DA
authors.lastname: Heerding
authors.forename: Chet
authors.initials: C
authors.lastname: Kwon
authors.forename: Stephen T
authors.initials: ST
authors.lastname: Ross
authors.forename: James M
authors.initials: JM
authors.lastname: Samanen
authors.forename: Dennis T
authors.initials: DT
authors.lastname: Takata
authors.forename: Irene N
authors.initials: IN
authors.lastname: Uzinskas
authors.forename: Catherine C K
authors.initials: CC
authors.lastname: Yuan
authors.forename: R Curtis
authors.initials: RC
authors.lastname: Haltiwanger
authors.forename: Catherine J
authors.initials: CJ
authors.lastname: Gress
authors.forename: Michael W
authors.initials: MW
authors.lastname: Lark
authors.forename: Shing Mei
authors.initials: SM
authors.lastname: Hwang
authors.forename: Ian E
authors.initials: IE
authors.lastname: James
authors.forename: David J
authors.initials: DJ
authors.lastname: Rieman
authors.forename: Robert N
authors.initials: RN
authors.lastname: Willette
authors.forename: Tian Li
authors.initials: TL
authors.lastname: Yue
authors.forename: Leonard M
authors.initials: LM
authors.lastname: Azzarano
authors.forename: Kevin L
authors.initials: KL
authors.lastname: Salyers
authors.forename: Brian R
authors.initials: BR
authors.lastname: Smith
authors.forename: Keith W
authors.initials: KW
authors.lastname: Ward
authors.forename: Kyung O
authors.initials: KO
authors.lastname: Johanson
authors.forename: William F
authors.initials: WF
authors.lastname: Huffman
mesh_terms: D000085:Acetates / Q000737:chemistry; D000284:Administration, Oral; D000631:Aminopyridines / Q000737:chemistry; D000818:Animals; D001682:Biological Availability; D002448:Cell Adhesion / Q000187:drug effects; D002460:Cell Line; D006207:Half-Life; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D010654:Phenylbutyrates / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology*; D051381:Rats
chemical_list: D000085:Acetates; D000631:Aminopyridines; D039302:Integrin alphaVbeta3; D010654:Phenylbutyrates; C121647:SB 265123