title: Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.
abstract: Parallel synthesis and iterative optimization led to the discovery of a series of potent and specific factor Xa inhibitors demonstrating excellent in vitro activity with promising pharmacokinetics.
authors.affiliation: Department of Medicinal Chemistry, Millennium Pharmaceuticals Inc., 256 East Grand Avenue, Suite 22, South San Francisco, CA 94080, USA. sbauer@portola.com
authors.forename: Shawn M
authors.initials: SM
authors.lastname: Bauer
authors.forename: Erick A
authors.initials: EA
authors.lastname: Goldman
authors.forename: Wenrong
authors.initials: W
authors.lastname: Huang
authors.forename: Ting
authors.initials: T
authors.lastname: Su
authors.forename: Lingyan
authors.initials: L
authors.lastname: Wang
authors.forename: John
authors.initials: J
authors.lastname: Woolfrey
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Wu
authors.forename: Jingmei F
authors.initials: JF
authors.lastname: Zuckett
authors.forename: Ann
authors.initials: A
authors.lastname: Arfsten
authors.forename: Brian
authors.initials: B
authors.lastname: Huang
authors.forename: Jaya
authors.initials: J
authors.lastname: Kothule
authors.forename: Joyce
authors.initials: J
authors.lastname: Lin
authors.forename: Bridget
authors.initials: B
authors.lastname: May
authors.forename: Uma
authors.initials: U
authors.lastname: Sinha
authors.forename: Paul W
authors.initials: PW
authors.lastname: Wong
authors.forename: Athiwat
authors.initials: A
authors.lastname: Hutchaleelaha
authors.forename: Robert M
authors.initials: RM
authors.lastname: Scarborough
authors.forename: Bing-Yan
authors.initials: BY
authors.lastname: Zhu
mesh_terms: D000990:Antithrombin III / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D065427:Factor Xa Inhibitors; D006801:Humans; D008968:Molecular Conformation; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D065427:Factor Xa Inhibitors; D000990:Antithrombin III