3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists

A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hE...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3504-3507
Hauptverfasser:	ZHAO, Shu-Hai, BERGER, Jacob, CLARK, Robin D, SETHOFER, Steven G, KRAUSS, Nancy E, BROTHERS, Julie M, MARTIN, Renee S, MISNER, Dinah L, SCHWAB, Dietmar, ALEXANDROVA, Ludmila
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Medical sciences Models, Chemical Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Oxazines - chemical synthesis Oxazines - pharmacology Pharmacology. Drug treatments Rats Receptors, Serotonin - drug effects Receptors, Serotonin - metabolism Serotonin Antagonists - chemical synthesis Serotonin Antagonists - pharmacology Serotoninergic system Structure-Activity Relationship
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Zusammenfassung:	A series of novel 3,4-dihydro-2H-benzo[1,4]oxazine derivatives has been designed and synthesized as 5-HT(6) receptor antagonists. Many of the compounds displayed subnanomolar affinities for the 5-HT(6) receptor and good brain penetration in rats. The relationship of structure and lipophilicity to hERG inhibition of this series of compounds is discussed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.12.093