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

Shawn M Bauer; Erick A Goldman; Wenrong Huang; Ting Su; Lingyan Wang; John Woolfrey; Yanhong Wu; Jingmei F Zuckett; Ann Arfsten; Brian Huang; Jaya Kothule; Joyce Lin; Bridget May; Uma Sinha; Paul W Wong; Athiwat Hutchaleelaha; Robert M Scarborough; Bing-Yan Zhu

doi:10.1016/j.bmcl.2004.05.033

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

Bioorg Med Chem Lett. 2004 Aug 2;14(15):4045-50. doi: 10.1016/j.bmcl.2004.05.033.

Authors

Shawn M Bauer¹, Erick A Goldman, Wenrong Huang, Ting Su, Lingyan Wang, John Woolfrey, Yanhong Wu, Jingmei F Zuckett, Ann Arfsten, Brian Huang, Jaya Kothule, Joyce Lin, Bridget May, Uma Sinha, Paul W Wong, Athiwat Hutchaleelaha, Robert M Scarborough, Bing-Yan Zhu

Affiliation

¹ Department of Medicinal Chemistry, Millennium Pharmaceuticals Inc., 256 East Grand Avenue, Suite 22, South San Francisco, CA 94080, USA. sbauer@portola.com

PMID: 15225723
DOI: 10.1016/j.bmcl.2004.05.033

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.

MeSH terms

Antithrombin III / chemical synthesis*
Antithrombin III / pharmacology
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Factor Xa Inhibitors*
Humans
Molecular Conformation
Molecular Structure
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Factor Xa Inhibitors
Antithrombin III