N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists

N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists

The design, synthesis and SAR of novel tetrahydrocarbazole derivatives having 5-HT6 receptor antagonist activity is presented. The racemic compound 15e was found to possess desirable pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2012-11, Vol.22 (22), p.6980-6985
Hauptverfasser: Nirogi, Ramakrishna V.S., Konda, Jagadishu Babu, Kambhampati, Ramasastry, Shinde, Anil, Bandyala, Thrinath Reddy, Gudla, Parandhama, Kandukuri, Kiran Kumar, Jayarajan, Pradeep, Kandikere, Vishwottam, Dubey, P.K.
Format: Artikel
Sprache:eng
Schlagworte:
5-HT6R
amines
Amines - chemical synthesis
Amines - chemistry
Amines - pharmacokinetics
animal models
Animals
antagonists
Biological and medical sciences
brain
Brain - metabolism
Carbazoles - chemical synthesis
Carbazoles - chemistry
Carbazoles - pharmacokinetics
Central nervous system
chemistry
cognition
Half-Life
Humans
Male
Medical sciences
Microsomes, Liver - metabolism
NORT
pharmacokinetics
Pharmacology. Drug treatments
Rats
Rats, Wistar
Receptors, Serotonin - chemistry
Receptors, Serotonin - metabolism
Serotonin Antagonists - chemical synthesis
Serotonin Antagonists - chemistry
Serotonin Antagonists - pharmacokinetics
Structure-Activity Relationship
Structure–activity relationships
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacokinetics
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Beschreibung
Zusammenfassung:The design, synthesis and SAR of novel tetrahydrocarbazole derivatives having 5-HT6 receptor antagonist activity is presented. The racemic compound 15e was found to possess desirable pharmacokinetic properties, adequate brain penetration and activity in animal models of cognition.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.06.002