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Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.

作者信息

Sawa Masaaki, Tateishi Hirotaka, Mizuno Kazuhiro, Harada Hiroshi, Oue Mayumi, Tsujiuchi Hiroshi, Furutani Yasuji, Kato Shiro

机构信息

Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, 33-94 Enoki-cho, Suita, Osaka 564-0053, Japan.

出版信息

Bioorg Med Chem Lett. 2004 Dec 20;14(24):5963-6. doi: 10.1016/j.bmcl.2004.09.054.

DOI:10.1016/j.bmcl.2004.09.054
PMID:15546708
Abstract

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.

摘要

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