2-(芳基磺酰基)吲哚-1,3-二酮的合成及其抗菌和抗凝血活性

M. Jeyachandran, P. Ramesh
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引用次数: 8

摘要

2-(芳基磺酰基)吲哚-1,3-二酮,早期由邻苯二甲酸二乙酯和芳基甲基磺酮通过Claisen缩合合成,被发现是有效的血液抗凝剂。为了寻找2-(芳基磺酰)吲哚-1,3-二酮的改进类似物,我们首次在吡啶-哌啶介质存在下,采用邻苯二酸酐和芳基磺酰乙酸酯之间的Knoevenagel反应合成了它们(7 a-f)。对合成的2-(芳基磺酰基)吲哚-1,3-二酮进行了抗菌和抗凝血活性评价,结果均为显著活性。
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Synthesis, Antimicrobial, and Anticoagulant Activities of 2-(Arylsulfonyl)indane-1,3-diones
2-(Arylsulfonyl)indane-1,3-diones, earlier synthesized by Claisen condensation involving diethyl phthalate and aryl methyl sulphones, are found to be potent blood anticoagulants. In search of improved analogs of 2-(arylsulfonyl)indane-1,3-dione, we have synthesized them (7 a-f) by a different route involving Knoevenagel reaction between phthalic anhydride and arylsulfonylacetates in the presence of pyridine-piperidine medium for the first time. The synthesized 2-(arylsulfonyl)indane-1,3-diones were evaluated for antimicrobial and anticoagulant activities and all of them registered significant activity.
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