| Literature DB >> 22928914 |
Hongbing Huang1, Daniel S La, Alan C Cheng, Douglas A Whittington, Vinod F Patel, Kui Chen, Thomas A Dineen, Oleg Epstein, Russell Graceffa, Dean Hickman, Y-H Kiang, Steven Louie, Yi Luo, Robert C Wahl, Paul H Wen, Stephen Wood, Robert T Fremeau.
Abstract
A structure- and property-based drug design approach was employed to identify aminooxazoline xanthenes as potent and selective human β-secretase inhibitors. These compounds exhibited good isolated enzyme, cell potency, and selectivity against the structurally related aspartyl protease cathepsin D. Our efforts resulted in the identification of a potent, orally bioavailable CNS penetrant compound that exhibited in vivo efficacy. A single oral dose of compound 11a resulted in a significant reduction of CNS Aβ40 in naive rats.Entities:
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Year: 2012 PMID： 22928914 DOI： 10.1021/jm300598e
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446