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5-HT(6) receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides

RO-04-6790 (6a) has been identified in a random screen for 5-HT(6) 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 logD p...

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Published in:	European journal of medicinal chemistry 2001-02, Vol.36 (2), p.165
Main Authors:	Bös, M, Sleight, A J, Godel, T, Martin, J R, Riemer, C, Stadler, H
Format:	Article
Language:	English
Subjects:	Animals Binding, Competitive Biological Availability Humans Memory Disorders - chemically induced Memory Disorders - drug therapy Protein Binding Pyrimidines Rats Receptors, Serotonin - metabolism Scopolamine Hydrobromide Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacokinetics Serotonin Antagonists - pharmacology Sulfanilamides - chemical synthesis Sulfanilamides - pharmacokinetics Sulfanilamides - pharmacology
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container_title	European journal of medicinal chemistry
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creator	Bös, M Sleight, A J Godel, T Martin, J R Riemer, C Stadler, H
description	RO-04-6790 (6a) has been identified in a random screen for 5-HT(6) 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 logD 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.
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source	Elsevier
subjects	Animals Binding, Competitive Biological Availability Humans Memory Disorders - chemically induced Memory Disorders - drug therapy Protein Binding Pyrimidines Rats Receptors, Serotonin - metabolism Scopolamine Hydrobromide Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacokinetics Serotonin Antagonists - pharmacology Sulfanilamides - chemical synthesis Sulfanilamides - pharmacokinetics Sulfanilamides - pharmacology
title	5-HT(6) receptor antagonists: lead optimisation and biological evaluation of N-aryl and N-heteroaryl 4-amino-benzene sulfonamides
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