MEDI 40 |
| The intriguing distribution of 5-HT6 receptors in the brain together with its role in the higher cognitive processes such as memory and more recently in obesity is well documented. 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. Our continuing efforts towards design and discovery of selective 5-HT6 antagonists have lead to the identification of novel rigidized tryptamine derivatives. The effective lead generation and optimization methods have resulted in a series of potent 5-HT6 receptor ligands with Ki in the range of 1 - 5 nM, when tested by the in-vitro radio-ligand binding techniques. Synthesis, physicochemical properties and in-vitro binding data along with SAR will be discussed.
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Poster Session
7:00 PM-9:00 PM, Sunday, August 19, 2007 BCEC -- Exhibit Hall - B2, Poster
Sci-Mix
Division of Medicinal Chemistry |
