Bioorganic & Medicinal Chemistry Letters 2011-11-15

Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.

Lorin A Thompson, Jianliang Shi, Carl P Decicco, Andrew J Tebben, Richard E Olson, Kenneth M Boy, Jason M Guernon, Andrew C Good, Ann Liauw, Changsheng Zheng, Robert A Copeland, Andrew P Combs, George L Trainor, Daniel M Camac, Jodi K Muckelbauer, Kimberley A Lentz, James E Grace, Catherine R Burton, Jeremy H Toyn, Donna M Barten, Jovita Marcinkeviciene, Jere E Meredith, Charles F Albright, John E Macor

Index: Bioorg. Med. Chem. Lett. 21(22) , 6909-15, (2011)

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Abstract

The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats.Copyright © 2011 Elsevier Ltd. All rights reserved.