N-Arylsulfonylindole derivatives as serotonin 5-HT6 receptor ligands

…, HB Broughton, M Knowles, G McAllister…

Index: Russell; Baker; Barden; Beer; Bristow; Broughton; Knowles; McAllister; Patel; Castro Journal of Medicinal Chemistry, 2001 , vol. 44, # 23 p. 3881 - 3895

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Citation Number: 105

Abstract

A series of N 1-arylsulfonyltryptamines were found to be potent ligands of the human serotonin 5-HT6 receptor with the 5-methoxy-1-benzenesulfonyl analogue (19) having the highest affinity. Additionally, it was discovered that a group such as 3-(3-methoxybenzyl)-1, 2, 4-oxadiazol-5-yl in the 2-position of the indole ring (43) can replace the arylsulfonyl substituent in the 1-position with no loss of affinity. This suggested that the binding ...