Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1374592 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.
Graphical abstractBrain-penetrable proline amides were developed as 5HT2c agonists with more than 1000-fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kevin K.-C. Liu, Bruce A. Lefker, Mark A. Dombroski, Phoebe Chiang, Peter Cornelius, Terrell A. Patterson, Yuan Zeng, Stephanie Santucci, Elizabeth Tomlinson, Colleen P. Gibbons, Ravi Marala, Janice A. Brown, Jimmy X. Kong, Eunsun Lee, Wendy Werner,