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Hydroxytriamides as potent gamma-secretase inhibitors |
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| Authors: | Prasad C V C Wallace Owen B Noonan Jeffrey W Sloan Charles P Lau Wai Vig Shikha Parker Michael F Smith David W Hansel Steven B Polson Craig T Barten Donna M Felsenstein Kevin M Roberts Susan B |
| Affiliation: | Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. prasad.chaturvedula@bms.com |
| Abstract: | Using a cell-based assay, we have identified optimal residues and key recognition elements necessary for inhibition of gamma-secretase. An (S)-hydroxy group or 3,5-difluorophenylacetyl group at the amino terminus and N-methyltertiary amide moiety at the carboxy terminus provided potent gamma-secretase inhibitors with an IC(50) <10 nM. |
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