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

  作者 Abdou, WM; Ganoub, NA; Geronikaki, A; Sabry, E  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2008年43-5;  页码  1015-1024  
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[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.

 
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