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Discovery of a potent M 5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2022 Dec 15; Vol. 78, pp. 129021. Date of Electronic Publication: 2022 Oct 10. - Publication Year :
- 2022
-
Abstract
- This Letter describes our ongoing effort to improve the clearance of selective M <subscript>5</subscript> antagonists. Herein, we report the replacement of the previously disclosed piperidine amide (4, disclosed in Part 1) with a pyrrolidine amide core. Several compounds within this series provided good potency, subtype selectivity, and low to moderate clearance profiles. Interestingly, the left-hand side SAR for this series diverged from our earlier efforts.<br />Competing Interests: Declaration of Competing Interest Some authors are inventors on application for composition of matter patents that protect several series of M(5) antagonists.<br /> (Copyright © 2022 Elsevier Ltd. All rights reserved.)
- Subjects :
- Kinetics
Muscarinic Antagonists
Amides pharmacology
Pyrrolidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 78
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 36228968
- Full Text :
- https://doi.org/10.1016/j.bmcl.2022.129021