Abdou Wafaa M, Ganoub Neven A, Geronikaki Athina, Sabry Eman
Pesticide Chemistry Department, National Research Centre, Elbohouth Street, D-12622 Dokki, Cairo, Egypt.
Eur J Med Chem. 2008 May;43(5):1015-24. doi: 10.1016/j.ejmech.2007.07.005. Epub 2007 Jul 27.
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).
让一系列取代亚芳基噻唑与维蒂希-霍纳（WH）试剂四乙基甲基-1,1-双膦酸酯反应，通过迈克尔加成反应根据实验条件以不同产率生成相应的杂芳基亚甲基双膦酸酯（BPs）。对新的BPs进行酸水解以获得相应的双膦酸。还根据构效关系（SAR）讨论了产物在大鼠佐剂模型中的预测和体内活性。
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