Synthesis and quantitative structure-activity relationship study of substituted imidazophosphor ester based tetrazolo[1,5-b] pyridazines as antinociceptive/anti-inflammatory agents

被引：13

作者：

Abdou, Wafaa M. ^{[1
]}

Ganoub, Neven A. ^{[1
]}

Sabry, Eman ^{[1
]}

机构：

[1] Natl Res Ctr, Chem Ind Div, Cairo, Egypt

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2013年 / 9卷

关键词：

antinociceptive/anti-inflammatory agents; imidazophosphor esters; phosphonyl carbanions; ring closure; tetrazolo[1,5-b] pyridazine; ALPHA-AMINOPHOSPHONATES; DUAL INHIBITORS; ALKYLIDENEPHOSPHORANES; BISPHOSPHONATES; CARBODIIMIDES; HETEROCYCLES;

D O I：

10.3762/bjoc.9.199

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A high-yielding general synthesis of imidazophosphor ester based tetrazolo[1,5-b]pyridazines is described. A conjugated reaction between 3,6-diazidopyridazine and different types of phosphonyl carbanion reagents followed by intramolecular cyclization afforded the target products, by using sodium ethanolate solution as a reaction medium. Among the products, five compounds, at a dose of 50 mg per kilogram body weight, showed a notable antinociceptive and anti-inflammatory activity without toxic side-effects.

引用

收藏

页码：1730 / 1736

页数：7

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