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J Med Chem. 2010 Mar 25;53(6):2521-7. doi: 10.1021/jm901674f.

5-Cyclic amine-3-arylsulfonylindazoles as novel 5-HT6 receptor antagonists.

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  • 1Wyeth Research, CN 8000, Princeton, New Jersey 08543, USA.


Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT(6) receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure-activity relationship of this potent class are discussed.

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