231287-75-5Relevant academic research and scientific papers
5-HT6 receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides
Boes, Michael,Sleight, Andrew J.,Godel, Thierry,Martin, James R.,Riemer, Claus,Stadler, Heinz
, p. 165 - 178 (2007/10/03)
RO-04-6790 (6a) has been identified in a random screen for 5-HT6 receptor antagonists. In a medicinal chemistry optimisation program a series of analogs comprising N-heteroaryl- and N-arylbenzenesulfonamides have been synthesised and investigated for their binding affinity. Compounds with a log D profile indicative of brain penetration have been subjected to in vivo testing for reversal of a scopolamine-induced retention deficit in a passive avoidance paradigm.
BENZOSULFONE DERIVATIVES
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, (2008/06/13)
The present invention relates to novel compounds of the general formula STR1 wherein R 1 is hydrogen;R. sup.2 is hydrogen, trifluoromethyl or lower alkyl;R 3 is hydrogen or amino; or R 1 and R 2 or R 3 and R 2 taken together are--CH. dbd.CH--CH=CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl; R 4, R 5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C. sub.3-C 6 cycloalkyl, C 3-C 6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group--NH(CH. sub.2). sub.n NR 6 R 7,--N(CH 3)(CH 2) n NR 6 R. sup.7,--NH(CH 2) n-morpholin-4-yl or--NH(CH 2) n OH; n is 2-4R 6 and R 7 are each independently hydrogen or lower alkyl,and to their pharmaceutically acceptable salts. It has been found that the compounds of formula I possess a selective affinity to 5HT-6 receptors.
