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Bioorg Med Chem Lett. 2012 Apr 15;22(8):2670-4. doi: 10.1016/j.bmcl.2012.03.014. Epub 2012 Mar 11.

Design and synthesis of potent, isoxazole-containing renin inhibitors.

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  • 1Merck Frosst Centre for Therapeutic Research, Kirkland, Québec, Canada.


The design and optimization of a novel isoxazole S(1) 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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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