Title of article
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity Original Research Article
Author/Authors
Joe A. Tran، نويسنده , , Fabio C. Tucci، نويسنده , , Wanlong Jiang، نويسنده , , Dragan Marinkovic، نويسنده , , Caroline W. Chen، نويسنده , , Melissa Arellano، نويسنده , , Stacy Markison، نويسنده , , Beth A. Fleck، نويسنده , , Jenny Wen، نويسنده , , Nicole S. White، نويسنده , , Joseph Pontillo، نويسنده , , John Saunders، نويسنده , , Daniel Marks، نويسنده , , Sam R. Hoare، نويسنده , , Ajay Madan، نويسنده , , Alan C. Foster، نويسنده , , Chen Chen، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
11
From page
5166
To page
5176
Abstract
A series of pyrrolidinones derived from phenylalanines were synthesized as potent antagonists of the human melanocortin-4 receptor. These compounds showed high potencies and selectivities, and several of them had good oral bioavailabilities. In addition, 12e demonstrated in vivo efficacy in a murine cachexia model.
Keywords
Pyrrolidinone , Synthesis , Melanocortin-4 receptor , Antagonist , Pharmacokinetics , Cachexia , Animal model
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2007
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305921
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