Tryptamine-based human β3-adrenergic receptor agonists.: Part 3:: Improved oral bioavailability via modification of the sulfonamide moiety
Tryptamine-based human β3-adrenergic receptor agonists.: Part 3:: Improved oral bioavailability via modification of the sulfonamide moiety
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DOI：
10.1016/j.bmcl.2004.12.033
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发表时间：
2005-02-15
影响因子：
2.7
通讯作者：
Kato, S
中科院分区：
文献类型：
--
作者：
Sawa, M;Mizuno, K;Kato, S
基于色胺的人β(3)-肾上腺素能受体（AR）激动剂的持续SAR研究被报道。先前的研究结果表明，2是一种有效的β (3)-AR激动剂。2中左侧芳基磺酰胺部分的进一步修饰提供了具有良好细胞渗透性的化合物，这些化合物对β (3)-AR具有强效的激动活性。肉桂胺类似物16i在体外具有良好的激动作用，在大鼠体内具有良好的口服生物利用度。(C) 2004 Elsevier Ltd.版权所有。
The continued SAR investigation of tryptamine-based human beta(3)-adrenergic receptor (AR) agonists is reported. Prior efforts resulted in the identification of 2 as a potent beta(3)-AR agonist. Further modification of the left side arylsulfonamide portion in 2 provided compounds with good cell permeability, which have potent agonistic activity for beta(3)-AR. Cinnamylamine analog 16i exhibited an excellent agonistic profile in vitro and good oral bioavailability in rats. (C) 2004 Elsevier Ltd. All rights reserved.