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4-氟苯甲酸酰肼与3-乙酰基-2,5-二取代-1,3,4-恶二唑啉的一些新型腙的合成及其抗菌活性

Synthesis and antimicrobial activity of some new hydrazones of 4-fluorobenzoic acid hydrazide and 3-acetyl-2,5-disubstituted-1,3,4-oxadiazolines.

作者信息

Rollas Sevim, Gulerman Nehir, Erdeniz Habibe

机构信息

Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Haydarpasa, Istanbul, Turkey.

出版信息

Farmaco. 2002 Feb;57(2):171-4. doi: 10.1016/s0014-827x(01)01192-2.

Abstract

A series of hydrazide hydrazones and 1,3,4-oxadiazolines of 4-fluorobenzoic acid hydrazide were prepared and evaluated as potential antimicrobial agents and were tested for their antibacterial and antifungal activities against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Candida albicans. From these compounds, 4-fluorobenzoic acid[(5-nitro-2-furanyl)methylene]hydrazide (1a) showed equal activity with ceftriaxone against S. aureus. In addition, the MIC values of compounds 1c, 1d and 2a for the same strain were in the range of those reported for ceftriaxone according to NCCLS 1997.

摘要

制备了一系列4-氟苯甲酸酰肼的酰腙和1,3,4-恶二唑啉,并将其作为潜在的抗菌剂进行评估,测试了它们对金黄色葡萄球菌、大肠杆菌、铜绿假单胞菌和白色念珠菌的抗菌和抗真菌活性。在这些化合物中,4-氟苯甲酸[(5-硝基-2-呋喃基)亚甲基]酰肼(1a)对金黄色葡萄球菌显示出与头孢曲松相当的活性。此外,根据1997年美国国家临床实验室标准化委员会(NCCLS)的报告,化合物1c、1d和2a对同一菌株的最低抑菌浓度(MIC)值在头孢曲松的报告范围内。

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