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Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors
Lorin A Thompson1, Jianliang Shi, Carl P Decicco
1Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. lorin.thompson@bms.com
Bioorganic & Medicinal Chemistry Letters
|October 7, 2011
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.
