MEDI 44 |
| Modulation of 5-HT receptors has been actively pursued for treatment of numerous disease states. Specifically, 5-HT6 receptor antagonists are being perceived for the treatment of CNS disorders and feeding disorders. Though highly selective and potent in-vitro ligands are available, the full characterization of functional and physiological usefulness of these compounds is limited due to the lack of desired brain penetration and pharmacokinetic properties required for the CNS agent. Keeping these factors in the mind we have designed 5-HT6 ligands on a chemically novel skeleton. The attempts have been made to impart the drug like properties to these molecules by optimizing their physicochemical properties. Our primary hit was found to have the Ki in the micromolar range. Our effective lead optimization strategies have resulted in the molecules with Ki in the range of 5 - 15 nM at the 5-HT6 receptor. Synthesis, physicochemical properties and the in-vitro binding data along with the SAR will be presented.
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Poster Session
7:00 PM-9:00 PM, Sunday, August 19, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Medicinal Chemistry |
