Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.
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.
Bauer
Shawn M
SM
Department of Medicinal Chemistry, Millennium Pharmaceuticals Inc., 256 East Grand Avenue, Suite 22, South San Francisco, CA 94080, USA. sbauer@portola.com
Goldman
Erick A
EA
Huang
Wenrong
W
Su
Ting
T
Wang
Lingyan
L
Woolfrey
John
J
Wu
Yanhong
Y
Zuckett
Jingmei F
JF
Arfsten
Ann
A
Huang
Brian
B
Kothule
Jaya
J
Lin
Joyce
J
May
Bridget
B
Sinha
Uma
U
Wong
Paul W
PW
Hutchaleelaha
Athiwat
A
Scarborough
Robert M
RM
Zhu
Bing-Yan
BY
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
D004791:Enzyme Inhibitors; D065427:Factor Xa Inhibitors; D000990:Antithrombin III