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Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012 |
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| Authors: | Melancon Bruce J Lamers Alexander P Bridges Thomas M Sulikowski Gary A Utley Thomas J Sheffler Douglas J Noetzel Meredith J Morrison Ryan D Scott Daniels J Niswender Colleen M Jones Carrie K Conn P Jeffrey Lindsley Craig W Wood Michael R |
| Institution: | Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA; Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, USA; Vanderbilt Specialized Chemistry Center for Probe Development (MLPCN), Nashville, TN 37232, USA. |
| Abstract: | This Letter describes the continued optimization of an MLPCN probe molecule (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at a more highly M(1)-selective antagonist, compound 13l (VU0415248). Muscarinic subtype selectivity across all five human and rat receptors for 13l, along with rat selectivity for the lead compound (ML012), is presented. |
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