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Published on: September 26, 2025
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012
Bruce J Melancon1, Thomas J Utley, Christian Sevel
1Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA. bruce.j.melancon@vanderbilt.edu
Abstract:
This Paper describes the continued optimization of an MLPCN probe molecule M(1) 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.
