A novel series of 3-ethoxyquinoxalin-2-carboxamides were designed as per the pharmacophoric requirements of 5-HT 3 receptor antagonist using ligand-based approach. The desired carboxamides were synthesized from the key intermediate, 3-ethoxyquinoxalin-2-carboxylic acid by coupling with appropriate a
Discovery of 2-substituted benzoxazole carboxamides as 5-HT3 receptor antagonists
β Scribed by Zhicai Yang; David J. Fairfax; Jun-Ho Maeng; Liaqat Masih; Alexander Usyatinsky; Carla Hassler; Soshanna Isaacson; Kevin Fitzpatrick; Russell J. DeOrazio; Jianqing Chen; James P. Harding; Matthew Isherwood; Svetlana Dobritsa; Kevin L. Christensen; Jonathan D. Wierschke; Brian I. Bliss; Lisa H. Peterson; Cathy M. Beer; Christopher Cioffi; Michael Lynch; W. Martin Rennells; Justin J. Richards; Timothy Rust; Yuri L. Khmelnitsky; Marlene L. Cohen; David D. Manning
- Publisher
- Elsevier Science
- Year
- 2010
- Tongue
- English
- Weight
- 391 KB
- Volume
- 20
- Category
- Article
- ISSN
- 0960-894X
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The serendipitous discovery of N-cyclohexyl-8-fluoro-3,3a,4,9b-tetrahydro-1H-thiochromeno[4,3-c]isoxazole-1-carboxamide as a selective human serotonin 5-HT 2B antagonist with K i of 42 Β± 5 nM is reported herein. A subsequent functional assay indicated little agonist activity compared to 5-HT itself.
## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a βFull Textβ option. The original article is trackable v
## Abstract A 5βHT~3~ receptor agonist based on a benzamide scaffold was identified in a screening of a small commercial compound library, and an elaborate SAR study originating from this hit was performed. The design, synthesis, and functional characterisation of benzamide analogues at the 5βHT~3~