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

被引:7
作者
Bauer, SM
Goldman, EA
Huang, WR
Su, T
Wang, LY
Woolfrey, J
Wu, YH
Zuckett, JMF
Arfsten, A
Huang, B
Kothule, J
Lin, J
May, B
Sinha, U
Wong, PW
Hutchaleelaha, A
Scarborough, RM
Zhu, BY
机构
[1] Millennium Pharmaceut Inc, Dept Med Chem, San Francisco, CA 94080 USA
[2] Millennium Pharmaceut Inc, Dept Biol, San Francisco, CA 94080 USA
[3] Millennium Pharmaceut Inc, Cardiovasc Res, San Francisco, CA 94080 USA
关键词
factor Xa; SAR; amino acid; aspartic acid;
D O I
10.1016/j.bmcl.2004.05.033
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4045 / 4050
页数:6
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