Title of article
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs
Author/Authors
Zhaozhong J. Jia، نويسنده , , Yanhong Wu، نويسنده , , Wenrong Huang، نويسنده , , Penglie Zhang، نويسنده , , Lane A. Clizbe، نويسنده , , Erick A. Goldman، نويسنده , , Uma Sinha، نويسنده , , Ann E. Arfsten، نويسنده , , Susan T. Edwards، نويسنده , , Merlyn Alphonso، نويسنده , , Athiwat Hutchaleelaha، نويسنده , , Robert M. Scarborough، نويسنده , , Bing-Yan Zhu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
7
From page
1221
To page
1227
Abstract
A variety of P4 motifs have been examined to increase the binding affinity and in vitro anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamide-based fXa inhibitors. Highly potent 2-naphthyl-P1 fXa inhibitors (Ki≤2 nM) with improved in vitro anticoagulant activity (2×TG≤1 μM) and respectable pharmacokinetic properties have been discovered.
Keywords
Factor Xa inhibitors.* Corresponding authors. Tel.: +1-650-246-7073 , fax: +1-650-246-
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794165
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