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Synthesis and biological evaluation of a novel structural type of serotonin 5-HT3 receptor antagonists
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:2769-2772
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- A series of novel 3-substituted quinoxalin-2-carboxamides were designed as per the pharmacophoric requirement for 5-HT(3) receptor antagonists and prepared by microwave irradiation and also by conventional method. The compounds were characterized by spectral data (IR, (1)H NMR, and MS) and the purity was ascertained by microanalysis. The synthesized compounds were evaluated for 5-HT(3) antagonisms in longitudinal muscle-myenteric plexus preparation from guinea pig ileum against 5-HT(3) agonist, 2-methyl-5-HT. Among the test compounds, N-{3-[(4-methylpiperazin-1-yl)methyl]-4-hydroxyphenyl}-3-methoxyquinoxalin-2-carboxamide 4e showed most favorable 5-HT(3) receptor antagonism.
- Subjects :
- Male
Agonist
medicine.drug_class
Stereochemistry
Guinea Pigs
Clinical Biochemistry
Pharmaceutical Science
Carboxamide
Biochemistry
Chemical synthesis
5-HT3 receptor
5-HT3 Receptor Antagonist
Drug Discovery
medicine
Animals
Serotonin 5-HT3 Receptor Antagonists
Serotonin Antagonists
Receptor
Molecular Biology
biology
Chemistry
Spectrum Analysis
Organic Chemistry
Biological activity
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....86a7afba2125ae957c28101e8f11222a