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Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.

Bioorganic & medicinal chemistry letters 2004 Aug 2; 14(15):4045-50

Link to PubMed abstract

Bauer S SM, Goldman E EA, Huang W W, Su T T, Wang L L, Woolfrey J J, Wu Y Y, Zuckett J JF, Arfsten A A, Huang B B, Kothule J J, Lin J J, May B B, Sinha U U, Wong P PW, Hutchaleelaha A A, Scarborough R RM, Zhu B BY

Department of Medicinal Chemistry, Millennium Pharmaceuticals Inc., 256 East Grand Avenue, Suite 22, South San Francisco, CA 94080, USA. sbauer@portola.com

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.