Homologation as a lead modification approach en route to a series of lactone-based muscarinic ligands |
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Authors: | Rong Gao Richie R. Bhandare Daniel J. Canney |
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Affiliation: | 1. Department of Pharmaceutical Sciences, Moulder Center for Drug Discovery Research, Temple University School of Pharmacy, 3307 N. Broad Street, Philadelphia, PA, 19140, USA
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Abstract: | Previous work identified the lactone ring as a useful scaffold for the design of muscarinic ligands and reported a lactone-based ligand with an IC50 of 340 nM. Using homologation as a lead modification approach, a new series of lactone-based compounds have been designed, synthesized, and screened in muscarinic binding assays. The approach provided a series of compounds with improved % inhibition values and identified the highest affinity lactone-based ligand reported to date. The results of these efforts and the structure–activity relationship for this series of lactones-based ligands are discussed. |
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