O-Methylasparvenone, a nitrogen-free serotonin antagonist

被引：25

作者：

Bos, M ^{[1
]}

Canesso, R

Inoue-Ohga, N

Nakano, A

Takehana, Y

Sleight, AJ

机构：

[1] F Hoffmann La Roche & Co Ltd, Preclin CNS Res, Div Pharma, CH-4070 Basel, Switzerland

[2] Nippon Roche Res Ctr, Dept Screening, Kamakura, Kanagawa 247, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1997年 / 5卷 / 12期

关键词：

D O I：

10.1016/S0968-0896(97)00160-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

O-Methylasparvenone (1) and asparvenone (2) were isolated from an Aspergillus parvulus Smith broth in a microbial screening for 5-HT2C ligands and found to be 5-HT2C antagonists. They represent the first nitrogen-free serotonin ligands. The absolute configuration of 1 was determined to be S by X-ray analysis of the corresponding Mosher-ester. A short and efficient synthesis of rac-1 was developed. This protocol was applied to the synthesis of derivatives of 1 and a structure-affinity relationship was established. (C) 1997 Elsevier Science Ltd.

引用

页码：2165 / 2171

页数：7

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