MEDI 29 |
| 5-HT6 receptor antagonists from SmithKline Beechame, Roche and recently from Dr. Esteve's lab have reported to reduce body weight and food intake in rats. However, in spite of their demonstrated efficacy in cognition as well as obesity, the lack of desirable pharmacokinetic properties required for these CNS agents is one of the main reasons for full characterization of functional and physiological usefulness of these molecules in human therapy. Part of ongoing programme at Suven for the synthesis of selective 5-HT6 ligands as antiobesity agents, we have designed a series of 3-(Amino)alkoxy indoles derivatives. Unlike the reported known ligands these compounds are conformationally highly flexible molecules. Our effective lead generation coupled with molecular modeling studies gave compounds with Ki in the range of 1 - 5 nM. The synthesis, in-vitro binding data along with SAR and in-vivo efficacy of the lead molecule will be presented.
|
|
Sci-Mix
8:00 PM-10:00 PM, Monday, August 20, 2007 BCEC -- Exhibit Hall - B2, Sci-Mix
Poster Session
Division of Medicinal Chemistry |
