Bioorganic and Medicinal Chemistry Letters p. 2670 - 2674 (2012)
Update date:2022-07-29
Topics:
Fournier, Pierre-André
Arbour, Mélissa
Cauchon, Elizabeth
Chen, Austin
Chefson, Amandine
Ducharme, Yves
Falgueyret, Jean-Pierre
Gagné, Sébastien
Grimm, Erich
Han, Yongxin
Houle, Robert
Lacombe, Patrick
Lévesque, Jean-Franois
MacDonald, Dwight
MacKay, Bruce
McKay, Dan
Percival, M. David
Ramtohul, Yeeman
St-Jacques, René
Toulmond, Sylvie
The design and optimization of a novel isoxazole S1 linker for renin inhibitor is described herein. This effort culminated in the identification of compound 18, an orally bioavailable, sub-nanomolar renin inhibitor even in the presence of human plasma. When compound 18 was found to inhibit CYP3A4 in a time dependent manner, two strategies were pursued that successfully delivered equipotent compounds with minimal TDI potential.
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Doi:10.1021/ic101041m
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