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Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors |
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| Authors: | Moore Keith P Zhu Hong Rajapakse Hemaka A McGaughey Georgia B Colussi Dennis Price Eric A Sankaranarayanan Sethu Simon Adam J Pudvah Nicole T Hochman Jerome H Allison Timothy Munshi Sanjeev K Graham Samuel L Vacca Joseph P Nantermet Philippe G |
| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. keith_moore2@merck.com |
| Abstract: | This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one case, potency was compromised in the process. |
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