Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
Bioorg Med Chem Lett
; 59: 128554, 2022 03 01.
Article
in En
| MEDLINE
| ID: mdl-35051575
ABSTRACT
Motilin is a 22-amino-acid gastrointestinal (GI) hormone and is involved in the regulation of GI motility through binding to GPR38, the motilin receptor which is expressed on smooth muscle cells in the GI tract. Therefore, GPR38 agonists are expected to be novel gastrointestinal prokinetic agents for the treatment of functional gastrointestinal disorders such as gastroparesis and chronic constipation. We identified a series of N-methylanilide derivatives as novel non-macrolide GPR38 agonists. Among them, 12 di-l-tartrate (DS-3801b) was selected as a clinical candidate for further evaluation.
Key words
Full text:
1
Database:
MEDLINE
Main subject:
Piperazines
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Gastrointestinal Agents
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Gastroparesis
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Cyclohexanes
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Receptors, G-Protein-Coupled
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Drug Discovery
/
Aniline Compounds
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2022
Type:
Article