Tryptamine-Based Human ?3-Adrenergic Receptor Agonists. Part 2. SAR of the Methylene Derivatives

Autor:	Yasuji Furutani, Hiroshi Tsujiuchi, Mayumi Oue, Masaaki Sawa, Kazuhiro Mizuno, Hirotaka Tateishi, Shiro Kato, Hiroshi Harada
Rok vydání:	2005
Předmět:	chemistry.chemical_classification Tryptamine chemistry.chemical_compound β3 adrenergic receptor chemistry Stereochemistry Chinese hamster ovary cell Subtype selectivity Moiety General Medicine Methylene Receptor Sulfonamide
Zdroj:	ChemInform. 36
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200515245
Popis:	A series of tryptamine derivatives with modified sulfonamide were designed, synthesized, and evaluated for their ability to stimulate cAMP accumulation in CHO cells expressing the cloned human beta3-adrenergic receptor (AR). For this series of compounds, our objective was to symmetrize the alpha-position of the tryptamine moiety maintaining its activity and reducing the cost of production. Compound 11h, having m-aminobenzene, exhibited excellent agonistic activity for beta3-AR with excellent subtype selectivity.
Databáze:	OpenAIRE
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