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以1-氯-3,4-二氢萘-2-甲醛为起始原料合成一些新型噻唑、噻唑烷酮和噻唑啉衍生物及其抗菌活性评价

Synthesis and antimicrobial evaluation of some new thiazole, thiazolidinone and thiazoline derivatives starting from 1-chloro-3,4-dihydronaphthalene-2-carboxaldehyde.

作者信息

Bondock Samir, Khalifa Wesam, Fadda Ahmed A

机构信息

Department of Chemistry, Faculty of Science, Mansoura University, El-gomhuria street, El-Dakhlia, ET-35516 Mansoura, Egypt.

出版信息

Eur J Med Chem. 2007 Jul;42(7):948-54. doi: 10.1016/j.ejmech.2006.12.025. Epub 2007 Jan 13.

Abstract

The thiosemicarbazones (3 and 6) and N-arylidene cyanoacetohydrazide (12) were prepared and used as key intermediates for the synthesis of 4-thiazolidinones (4, 5, 7-9), thiazoles (10a,b and 11a-d) and thiazoline (13) derivatives. Treatment of 13 with a mixture of triethylorthoformate and acetic anhydride afforded thiazolo[5,4-d]pyrimidinone derivative (14). The newly synthesized compounds were characterized by IR, (1)H NMR and mass spectral studies. Representative compounds of the synthesized products were tested and evaluated as antimicrobial agents.

摘要

制备了缩氨基硫脲(3和6)及N - 亚芳基氰基乙酰肼(12),并将其用作合成4 - 噻唑烷酮(4、5、7 - 9)、噻唑(10a、b和11a - d)及噻唑啉(13)衍生物的关键中间体。用原甲酸三乙酯和乙酸酐的混合物处理13,得到噻唑并[5,4 - d]嘧啶酮衍生物(14)。通过红外光谱、核磁共振氢谱和质谱研究对新合成的化合物进行了表征。对合成产物的代表性化合物作为抗菌剂进行了测试和评估。

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