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抗菌和抗真菌剂的研究。十三。1-芳基甲基-4-芳基-1H-吡咯-3-羧酸的合成及抗菌活性

Research on antibacterial and antifungal agents. XIII. Synthesis and antimicrobial activity of 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acids.

作者信息

Massa S, Di Santo R, Mai A, Botta M, Artico M, Panico S, Simonetti G

机构信息

Dipartimento di Studi Farmaceutici, Università di Roma La Sapienza, Italy.

出版信息

Farmaco. 1990 Jul;45(7-8):833-46.

PMID:2282118
Abstract

Several 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylic acid derivatives have been synthetized and tested as antifungal and antibacterial agents. Reaction between tosylmethylisocyanide (TosMIC) and beta-arylacrylic esters under basic conditions furnished 4-aryl-1H-pyrrole-3-carboxylic esters, which were then benzylated at 1 position. Alkaline hydrolysis of ethyl 1-arylmethyl-4-aryl-1H-pyrrole-3-carboxylates afforded the title compounds. All tested derivatives were found to be inactive as antifungal agents. Some of them showed appreciable antibacterial activities against Staphylococcus spp.

摘要

已经合成了几种1-芳基甲基-4-芳基-1H-吡咯-3-羧酸衍生物，并作为抗真菌和抗菌剂进行了测试。对甲苯磺酰甲基异氰化物（TosMIC）与β-芳基丙烯酸酯在碱性条件下反应生成4-芳基-1H-吡咯-3-羧酸酯，然后在1位进行苄基化。1-芳基甲基-4-芳基-1H-吡咯-3-羧酸乙酯的碱性水解得到标题化合物。所有测试的衍生物均被发现作为抗真菌剂无活性。其中一些对葡萄球菌属表现出明显的抗菌活性。

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