title: Design, synthesis, and SAR of amino acid derivatives as factor Xa inhibitors.
abstract: A series of potent and selective factor Xa inhibitors was synthesized using various readily available amino acids as central templates. The most potent compound displays IC(50) of 3 nM.
authors.affiliation: COR Therapeutics, Inc., 256 East Grand Avenue, South San Francisco, CA 94080, USA. tsu@corr.com
authors.forename: T
authors.initials: T
authors.lastname: Su
authors.forename: Y
authors.initials: Y
authors.lastname: Wu
authors.forename: B
authors.initials: B
authors.lastname: Doughan
authors.forename: Z J
authors.initials: ZJ
authors.lastname: Jia
authors.forename: J
authors.initials: J
authors.lastname: Woolfrey
authors.forename: B
authors.initials: B
authors.lastname: Huang
authors.forename: P
authors.initials: P
authors.lastname: Wong
authors.forename: G
authors.initials: G
authors.lastname: Park
authors.forename: U
authors.initials: U
authors.lastname: Sinha
authors.forename: R M
authors.initials: RM
authors.lastname: Scarborough
authors.forename: B Y
authors.initials: BY
authors.lastname: Zhu
mesh_terms: D015195:Drug Design; D065427:Factor Xa Inhibitors; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D065427:Factor Xa Inhibitors; D015842:Serine Proteinase Inhibitors