Literature DB >> 20202843

Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity.

Kevin K-C Liu1, 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, Zane Wenzel, Craig Giragossian, Hou Chen, Steven B Coffey.   

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. 2010. Published by Elsevier Ltd.

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Year:  2010        PMID: 20202843     DOI: 10.1016/j.bmcl.2010.01.107

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Authors:  Guy Rouquet; Dianna E Moore; Malcolm Spain; Daniel M Allwood; Claudio Battilocchio; David C Blakemore; Paul V Fish; Stephen Jenkinson; Alan S Jessiman; Steven V Ley; Gordon McMurray; R Ian Storer
Journal:  ACS Med Chem Lett       Date:  2015-01-20       Impact factor: 4.345

  1 in total

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