- Synthesis and structure activity relationship of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives as 5-HT6 receptor antagonists
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As part of our efforts to develop better therapies for the treatment of cognitive impairment associated with Alzheimer's disease and Schizophrenia, we have focused our research towards 5-HT6 receptor (5-HT6R) in order to identify potent and selective ligands for this purpose. Herein, we report the synthesis, structure activity relationship and biological evaluation of a novel series of 3-(arylsulfonyl)-8- (piperidin-4-yl amino)quinoline derivatives, as 5-HT6 receptor (5-HT6R) antagonists. In this work, we have shown that moving from aryl sulfonamide platform to biaryl sulfone platform retains the 5-HT6.R affinity when tested in vitro in cell based reporter gene functional assay.
- Nirogi, Ramakrishna V.S.,Badange, Rajeshkumar,Gudla, Parandhama,Khagga, Mukkanti
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p. 3779 - 3784
(2014/08/05)
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- QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR
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The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X', Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.
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Page/Page column 57
(2009/04/25)
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