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Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M1 positive allosteric modulators |
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| Authors: | Feng V. Yang William D. Shipe Jaime L. Bunda M. Brad Nolt David D. Wisnoski Zhijian Zhao James C. Barrow William J. Ray Lei Ma Marion Wittmann Matthew A. Seager Kenneth A. Koeplinger George D. Hartman Craig W. Lindsley |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA;2. Department of Alzheimer’s Research, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA;3. Department of Drug Metabolism, Merck Research Laboratories, 770 Sumneytown Pike, PO Box 4, West Point, PA 19486, USA |
| Abstract: | An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M1 positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified. |
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