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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Bibliographic Details
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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Summary: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.
ISSN:0223-5234