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Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2022 Mar 01; Vol. 59, pp. 128554. Date of Electronic Publication: 2022 Jan 18. - Publication Year :
- 2022
-
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.<br /> (Copyright © 2022 Elsevier Ltd. All rights reserved.)
- Subjects :
- Aniline Compounds chemistry
Animals
Cyclohexanes chemical synthesis
Cyclohexanes chemistry
Dose-Response Relationship, Drug
Gastrointestinal Agents chemical synthesis
Gastrointestinal Agents chemistry
Gastroparesis metabolism
Humans
Molecular Structure
Piperazines chemical synthesis
Piperazines chemistry
Rabbits
Receptors, G-Protein-Coupled metabolism
Structure-Activity Relationship
Aniline Compounds pharmacology
Cyclohexanes pharmacology
Drug Discovery
Gastrointestinal Agents pharmacology
Gastroparesis drug therapy
Piperazines pharmacology
Receptors, G-Protein-Coupled agonists
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 59
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 35051575
- Full Text :
- https://doi.org/10.1016/j.bmcl.2022.128554