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Bioorg Med Chem Lett. 2004 Dec 20;14(24):5963-6.

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

Author information

1
Chemistry Research Laboratories, Dainippon Pharmaceutical Co., Ltd, 33-94 Enoki-cho, Suita, Osaka 564-0053, Japan. masaaki-sawa@dainippon-pharm.co.jp

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.

PMID:
15546708
DOI:
10.1016/j.bmcl.2004.09.054
[Indexed for MEDLINE]

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