Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377435 | Bioorganic & Medicinal Chemistry Letters | 2007 | 6 Pages |
Abstract
This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane derivative 3j had potent anticoagulant activity as well as anti-fXa activity. Synthetic study of the optical isomers of 3g demonstrated that (−)-3g had more potent activity.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Tsutomu Nagata, Toshiharu Yoshino, Noriyasu Haginoya, Kenji Yoshikawa, Yumiko Isobe, Taketoshi Furugohri, Hideyuki Kanno,