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J Med Chem. 2006 Oct 19;49(21):6147-50.

Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.

Author information

  • 1Department of Medicinal Chemistry, Biological Chemistry, Molecular Systems and Structural Biology Merck Research Laboratories, Post Office Box 4, West Point, Pennsylvania 19486, USA. shawn_stachel@merck.com

Erratum in

  • J Med Chem. 2006 Nov 30;49(24):7252. Wu, Guoxin [added]; Crouthamel, Michelle [added].


A macrocyclic inhibitor of beta-secretase was designed by covalently cross-linking the P1 and P3 side chains of an isophthalamide-based inhibitor. Macrocyclization resulted in significantly improved potency and physical properties when compared to the initial lead structures. More importantly, these macrocyclic inhibitors also displayed in vivo amyloid lowering when dosed in a murine model.

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