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Eur J Med Chem. 2008 May;43(5):1015-24. Epub 2007 Jul 27.

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

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  • 1Pesticide Chemistry Department, National Research Centre, Elbohouth Street, D-12622 Dokki, Cairo, Egypt.


A series of substituted arylidene thiazoles were allowed to react with Wittig-Horner (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).

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