SYNTHESIS OF METABOLICALLY STABLE ARYLPIPERAZINE 5-HT1A RECEPTOR AGONISTS

被引：26

作者：

ROMERO, AG ^{[1
]}

DARLINGTON, WH ^{[1
]}

PIERCEY, MF ^{[1
]}

LAHTI, RA ^{[1
]}

机构：

[1] UPJOHN CO,CNS DIS RES,KALAMAZOO,MI 49001

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1992年 / 2卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(00)80460-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Although N-alkylarylpiperazines as a class are finding use as anxiolytics and antidepressants, many of these arylpiperazines are highly metabolically labile at the n-alkyl-piperazine bond. We have found that cyclopropanating the n-butyl chain contained in the 5-HT1A receptor agonist ipsapirone (2) instills a resistance to this metabolism as well as providing information about the geometrical requirements of the 5-HT1A receptor.

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页码：1703 / 1706

页数：4

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