PREPARATION, STRUCTURAL-ANALYSIS AND ANTICONVULSANT ACTIVITY OF 3-AMINOPYRAZOLE AND 5-AMINOPYRAZOLE N-BENZOYL DERIVATIVES

被引：72

作者：

MICHON, V ^{[1
]}

DUPENHOAT, CH ^{[1
]}

TOMBRET, F ^{[1
]}

GILLARDIN, JM ^{[1
]}

LEPAGE, F ^{[1
]}

BERTHON, L ^{[1
]}

机构：

[1] ECOLE NORMALE SUPER, DEPT CHIM, URA 1679, F-75231 PARIS 05, FRANCE

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1995年 / 30卷 / 02期

关键词：

BENZAMIDE; AMINOPYRAZOLE; ANTICONVULSANT ACTIVITY; NMR; SELECTIVE LONG-RANGE HETERONUCLEAR CORRELATIONS; STEADY-STATE NUCLEAR OVERHAUSER EFFECT;

D O I：

10.1016/0223-5234(96)88220-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Some unsymmetrical N-exocyclic and N-endocyclic derivatives from benzoylation of 3- and 5-aminopyrazole were prepared with the aim of comparing their anticonvulsant activity towards the MES and scMET tests. Unambiguous proof of their structure was obtained from heteronuclear long-range correlation spectroscopy and NOE difference spectra, Only the N-exo-pyrazole benzamides showed good protection with respect to these tests.

引用

页码：147 / 155

页数：9

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