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Bruce Melancon

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Organization: Vanderbilt University
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Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012
Co-reporter:Bruce J. Melancon, Thomas J. Utley, Christian Sevel, Margrith E. Mattmann, Yiu-Yin Cheung, Thomas M. Bridges, Ryan D. Morrison, Douglas J. Sheffler, Colleen M. Niswender, J. Scott Daniels, P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood
Bioorganic & Medicinal Chemistry Letters 2012 Volume 22(Issue 15) pp:5035-5040
Publication Date(Web):1 August 2012
DOI:10.1016/j.bmcl.2012.06.018
This Paper describes the continued optimization of an MLPCN probe molecule M1 antagonist (ML012) through an iterative parallel synthesis approach. After several rounds of modifications of the parent compound, we arrived at a new azetidine scaffold that displayed improved potency while maintaining a desirable level of selectivity over other muscarinic receptor subtypes. Data for representative molecules 7w (VU0452865) and 12a (VU0455691) are presented.
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