1247087-25-7Relevant articles and documents
Design and synthesis of potent, isoxazole-containing renin inhibitors
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
, p. 2670 - 2674 (2012/05/31)
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.
