Title of article
Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors
Author/Authors
Hiroshi Ueno ، نويسنده , , Katsuyuki Yokota، نويسنده , , Jun-ichi Hoshi، نويسنده , , Katsutaka Yasue، نويسنده , , Mikio Hayashi، نويسنده , , Itsuo Uchida، نويسنده , , Kazuo Aisaka، نويسنده , , Yasunori Hase، نويسنده , , Susumu Katoh، نويسنده , , Hidetsura Cho، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
185
To page
189
Abstract
A series of novel 2,7-disubstituted tetrahydroisoquinoline derivatives were designed and synthesized. Among these derivatives, compounds 1 and 2 (JTV-803) exhibited potent inhibitory activity against FXa and good selectivity with respect to other serine proteases (thrombin, plasmin, and trypsin). In addition, compound 2 exhibited potent anti-FXa activity after intravenous and oral administration to cynomolgus monkey, and showed a dose-dependent antithrombotic effect in a rat model of venous thrombosis.
Keywords
Tetrahydroisoquinoline derivatives , Potent and selective factor Xa (FXa) inhibitor , JTV-803 , Antithrombotic effect on venous thrombosis in rats , Inhibition of human Fxa
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795176
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