Discovery of novel tetrahydroisoquinoline derivatives as potent and selective factor Xa inhibitors
…, M Hayashi, I Uchida, K Aisaka, Y Hase, S Katoh…
Index: Ueno, Hiroshi; Yokota, Katsuyuki; Hoshi, Jun-Ichi; Yasue, Katsutaka; Hayashi, Mikio; Uchida, Itsuo; Aisaka, Kazuo; Hase, Yasunori; Katoh, Susumu; Cho, Hidetsura Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 1 p. 185 - 189
Full Text: HTML
Citation Number: 6
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- ...
Related Articles:
Highly potent and selective zwitterionic agonists of the δ-opioid receptor. Part 1
[Middleton, Donald S.; Maw, Graham N.; Challenger, Clare; Jessiman, Alan; Johnson, Patrick S.; Million, William A.; Nichols, Carly L.; Price, Jenny A.; Trevethick, Michael Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 4 p. 905 - 910]
[Ueno, Hiroshi; Yokota, Katsuyuki; Hoshi, Jun-Ichi; Yasue, Katsutaka; Hayashi, Mikio; Hase, Yasunori; Uchida, Itsuo; Aisaka, Kazuo; Katoh, Susumu; Cho, Hidetsura Journal of Medicinal Chemistry, 2005 , vol. 48, # 10 p. 3586 - 3604]