Rigidized 1-aryl sulfonyl tryptamines: Synthesis and pharmacological evaluation as 5-HT6 receptor ligands

Cognitive Enhancers (Nootropics). Part 1: Drugs Interacting with Receptors

“…The medicinal chemistry was described [492]. The effects to ameliorate scopolamine-induced memory deficits in object recognition and object location tasks in Wistar rats were reported [493] Novel chemical classes of 5-HT 6 receptor antagonists, i.e., aryl aminosulfonamide derivatives with a K b of 0.02 nM were reported by medicinal chemists at Suven, as were N 1 -arylsulfonyl-3-piperazinyl indole derivatives with a K i of 3.4 nM [494][495][496][497][498][499][500][501].…”

Synthesis and biological evaluation of novel N1-phenylsulphonyl indole derivatives as potent and selective 5-HT6R ligands for the treatment of cognitive disorders

“…During this decade or so, there was a plenty of chemistry developed around different nuclei including the indole-based ones or even much simpler biphenyl sulfones and sulfonamides [16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32][33]34 ( Figure 2). Suven has reported several series of 1-sulfonylindoles bearing the amino group at 3 or 4 or 5 position of the central core [31][32][33] .…”

“…Suven has reported several series of 1-sulfonylindoles bearing the amino group at 3 or 4 or 5 position of the central core [31][32][33] . As part of our continuing research efforts in the 5-HT 6 area to identify potent and selective 5-HT 6 receptor ligands as potential treatments for cognitive dysfunction, we have attempted structural modification of earlier reported piperazinyl methyl-N 1 -phenylsulfonyl indole derivatives 33 .…”

[3-[(1-Methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indoles: Synthesis, SAR and biological evaluation as a novel class of 5-HT6 Receptor Antagonists

“…7 * For correspondence SB-742457, A 8 and Lu AE58054, B 9 are the two advanced stage 5-HT 6 R antagonists that have completed phase II clinical trials. Modification in the side chain of N-arylsulfonyl tryptamine, for e.g., MS-245, C, 10 a known 5-HT 6 R antagonist has led to the discovery of structurally diverse compounds as depicted by structures D 11 (reported by our research group) and E 12 which are potent 5-HT 6 R antagonists. In general, these compounds are characterized by having the cyclic amine moiety on indole nucleus.…”