Synthesis, properties, and perspectives of gem-diphosphono substituted-thiazoles

被引：13

作者：

Abdou, Wafaa M. ^{[1
]}

Ganoub, Neven A. ^{[1
]}

Geronikaki, Athina ^{[2
]}

Sabry, Ernan ^{[1
]}

机构：

[1] Natl Res Ctr, Dept Pesticide Chem, D-12622 Cairo, Egypt

[2] Univ Thessaloniki, Sch Pharm, GR-54006 Thessaloniki, Greece

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 43卷 / 05期

关键词：

drug research; chronic inflammation; bone resorption; heteroarylmethylene-1,1-bisphosphonates; alpha-phosphonate carbanions;

D O I：

10.1016/j.ejmech.2007.07.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted arylidene thiazoles were allowed to react with Wittig-Homer (WH) reagent, tetraethyl methyl-1,1-bisphosphonate, to produce via Michael addition reaction the corresponding heteroarylmethylenebisphosphonates (BPs) in different yields according to the experimental conditions. Acid hydrolysis of the new BPs was undertaken to obtain the corresponding bisphosphonic acids. Prediction and the in vivo activity of the products in the rat adjuvant model are also discussed in terms of structure-activity relationships (SAR). (C) 2007 Elsevier Masson SAS. All rights reserved.

引用

页码：1015 / 1024

页数：10

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