发现一种基于螺环吲哚烷的化合物，作为一种强效、选择性、口服生物利用度的黑皮质素受体 4 亚型激动剂。

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

机构信息

Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.

出版信息

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19.

DOI:10.1016/j.bmcl.2010.02.058

PMID:20207541

Abstract

We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.

摘要

我们报告了螺吲哚烷类化合物 1 的设计、合成和性质，这是一种有效的、选择性的、口服生物利用度的、非肽类黑皮质素 4 受体激动剂。化合物 1 在啮齿动物模型中表现出优异的勃起功能增强活性。

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发现一种基于螺环吲哚烷的化合物，作为一种强效、选择性、口服生物利用度的黑皮质素受体 4 亚型激动剂。

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

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发现一种基于螺环吲哚烷的化合物，作为一种强效、选择性、口服生物利用度的黑皮质素受体 4 亚型激动剂。

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.

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出版信息

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