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无溶剂微波合成及嘧啶并[4,5 - b] - 和吡唑并[3,4 - b]喹啉抗菌活性的评估

Solvent free microwave synthesis and evaluation of antimicrobial activity of pyrimido[4,5-b]- and pyrazolo[3,4-b]quinolines.

作者信息

Selvi Senniappan Thamarai, Nadaraj Vetrivel, Mohan Sellappan, Sasi Raju, Hema Manoharan

机构信息

Department of Chemistry (PG and Research), Kongunadu Arts and Science College, G.N. Mills Post, Coimbatore 641029, India.

出版信息

Bioorg Med Chem. 2006 Jun 1;14(11):3896-903. doi: 10.1016/j.bmc.2006.01.048. Epub 2006 Feb 7.

DOI:10.1016/j.bmc.2006.01.048
PMID:16464602
Abstract

A series of 2-oxopyrimido[4,5-b]-, 2-thio[4,5-b]-, 1-(p-tosyl)pyrazolo[3,4-b]- and 1-(2',4'-dinitrophenyl)pyrazolo[3,4-b]-quinolines have been synthesized in good to excellent yields by environmentally benign solvent free microwave-induced techniques involving the condensation of 2-chloro-3-formylquinolines with urea, thiourea, p-toluenesulfonylhydrazide and 2,4-dinitrophenylhydrazine, respectively, using PTSA as a catalyst. All the synthesized compounds were evaluated for their antibacterial and antifungal activities. Most of the compounds showed the best activity against Escherichia coli and Pseudomonas aeruginosa.

摘要

通过环境友好的无溶剂微波诱导技术,分别使用对甲苯磺酸(PTSA)作为催化剂,使2-氯-3-甲酰基喹啉与尿素、硫脲、对甲苯磺酰肼和2,4-二硝基苯肼缩合,已合成了一系列2-氧代嘧啶并[4,5-b]-、2-硫代[4,5-b]-、1-(对甲苯磺酰基)吡唑并[3,4-b]-和1-(2',4'-二硝基苯基)吡唑并[3,4-b]-喹啉,产率良好至优异。对所有合成的化合物进行了抗菌和抗真菌活性评估。大多数化合物对大肠杆菌和铜绿假单胞菌表现出最佳活性。

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