STRUCTURE ACTIVITY RELATIONSHIP OF QUINAZOLINEDIONE INHIBITORS OF CALCIUM-INDEPENDENT PHOSPHODIESTERASE

被引：86

作者：

LOWE, JA

ARCHER, RL

CHAPIN, DS

CHENG, JB

HELWEG, D

JOHNSON, JL

KOE, BK

LEBEL, LA

MOORE, PF

NIELSEN, JA

RUSSO, LL

SHIRLEY, JT

机构：

[1] Central Research Division Pfizer, Inc., Groton, Connecticut 06340, Eastern Point Road

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 02期

关键词：

D O I：

10.1021/jm00106a024

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of quinazolinediones and azaquinazolinediones is described which possess potent inhibitory activity toward the calcium-independent phosphodiesterase enzyme (CaIPDE). In vivo testing showed that this in vitro activity translates to animal models predictive of chronic diseases such as depression and inflammation. These results support the hypothesis that inhibition of CaIPDE may lead to useful activity in such chronic diseases.

引用

页码：624 / 628

页数：5

共 20 条

[1]

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[2]

ASKEW BM, 1963, LIFE SCI, V4, P725

[3] ASSESSMENT OF SELECTIVE-INHIBITION OF RAT CEREBRAL CORTICAL CALCIUM-INDEPENDENT AND CALCIUM-DEPENDENT PHOSPHODIESTERASES IN CRUDE EXTRACTS USING DEOXYCYCLIC AMP AND POTASSIUM-IONS [J].