Synthesis and pharmacological evaluation of a set of N-[2-(alkylamino)ethyl]benzotriazol-X-yl isobutyramides acting as local anesthetics

被引：19

作者：

Caliendo, G

Greco, G

Grieco, P

Raso, GM

Meli, R

Novellino, E

Perissutti, E

Santagada, V

机构：

[1] UNIV SALERNO,FAC FARM,I-84084 SALERNO,ITALY

[2] UNIV NAPLES FEDERICO II,FAC FARM,DIPARTIMENTO CHIM FARMACEUT & TOSSICOL,I-80138 NAPLES,ITALY

[3] UNIV NAPLES FEDERICO II,FAC FARM,DIPARTIMENTO FARM SPERIMENTALE,I-80138 NAPLES,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 31卷 / 02期

关键词：

benzotriazole; local anesthetic; acute toxicity; QSAR; lipophilicity;

D O I：

10.1016/0223-5234(96)80442-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A set of N-[2-(alkylamino)ethyl]benzotriazol-X-yl isobutyramides have been synthesized and assayed in vivo for their local anesthetic activity and acute toxicity. Some of them showed a more favorable pharmacological profile than that of the reference drug lidocaine. QSAR studies have delineated the influence of overall lipophilicity on surface and infiltration anesthetic activities.

引用

页码：99 / 104

页数：6

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