Article ; Online: Design and preparation of N-linked hydroxypyridine-based APJ agonists.
Bioorganic & medicinal chemistry letters
2022 Volume 73, Page(s) 128882
Abstract: Agonism of the apelin receptor (APJ) has demonstrated beneficial effects in models of heart failure. We have previously disclosed compounds such as 4, which showed good APJ agonist activity but were metabolized to the mono-demethylated, non- ... ...
| Abstract | Agonism of the apelin receptor (APJ) has demonstrated beneficial effects in models of heart failure. We have previously disclosed compounds such as 4, which showed good APJ agonist activity but were metabolized to the mono-demethylated, non-interconverting atropisomer metabolites. Herein, we detail the design and optimization of a novel series of N-linked APJ agonists with good potency, metabolic stability, and rat pharmacokinetic profile, which are unable to undergo the same metabolic mono-demethylation cleavage. |
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| MeSH term(s) | Animals ; Apelin ; Apelin Receptors/agonists ; Pyridines ; Rats ; Receptors, G-Protein-Coupled/agonists | |||||
| Chemical Substances | Apelin ; Apelin Receptors ; Pyridines ; Receptors, G-Protein-Coupled ; hydroxypyridines | |||||
| Language | English | |||||
| Publishing date | 2022-07-08 | |||||
| Publishing country | England | |||||
| Document type | Journal Article | |||||
| ZDB-ID | 1063195-1 | |||||
| ISSN | 1464-3405 ; 0960-894X | |||||
| ISSN (online) | 1464-3405 | |||||
| ISSN | 0960-894X | |||||
| DOI | 10.1016/j.bmcl.2022.128882 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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