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Bioorg. Med. Chem. Lett. · Mar 2014
Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.
- Scott D Kuduk, Christina N Di Marco, Jonathan R Saffold, William J Ray, Lei Ma, Marion Wittmann, Kenneth A Koeplinger, Charles D Thompson, George D Hartman, Mark T Bilodeau, and Douglas C Beshore.
- Department of Medicinal Chemistry, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA. Electronic address: scott_d_kuduk@merck.com.
- Bioorg. Med. Chem. Lett. 2014 Mar 1; 24 (5): 1417-20.
AbstractA series of methoxynaphthalene amides were prepared and evaluated as alternatives to quinolizidinone amide M1 positive allosteric modulators. A methoxy group was optimal for M1 activity and addressed key P-gp issues present in the aforementioned quinolizidinone amide series. Copyright © 2014 Elsevier Ltd. All rights reserved.
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