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环酰胺衍生物的合成、抗菌活性和对线虫的毒性。

Synthesis, antimicrobial activity and toxicity to nematodes of cyclam derivatives.

机构信息

Centro de Química Estrutural, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, 1049-001 Lisbon, Portugal.

iBB-Instituto de Bioengenharia e Biociências, Departamento de Bioengenharia, Instituto Superior Técnico, Universidade de Lisboa, Av. Rovisco Pais 1, Torre Sul, Piso 6, 1049-001 Lisbon, Portugal.

出版信息

Int J Antimicrob Agents. 2017 May;49(5):646-649. doi: 10.1016/j.ijantimicag.2017.03.002. Epub 2017 Mar 16.

DOI:10.1016/j.ijantimicag.2017.03.002
PMID:28315730
Abstract

The antimicrobial activity and toxicity to nematodes of the cyclam salt H{H(PhCH)Cyclam}⋅(CHCOOH) were evaluated. Estimated minimum inhibitory concentrations (MICs) of 9, 261 and 15 µg/mL were obtained for Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus, respectively. For selected Candida spp., the estimated MICs obtained ranged from 32 µg/mL to 63 µg/mL. Bactericidal activity was demonstrated but the compound was not reliably fungicidal. Concentrations of the cyclam salt up to 32 µg/mL did not significantly affect survival of the nematode Caenorhabditis elegans; however, concentrations equal or above this value significantly affected nematode survival in a dose-dependent manner.

摘要

评估了H{H(PhCH)Cyclam}⋅(CHCOOH)环脒盐对线虫的抗菌活性和毒性。分别获得了大肠杆菌、铜绿假单胞菌和金黄色葡萄球菌的最小抑菌浓度(MIC)估计值为 9、261 和 15μg/mL。对于选定的念珠菌属 spp.,获得的 MIC 值范围为 32μg/mL 至 63μg/mL。该化合物表现出杀菌活性,但不能可靠地杀菌。环脒盐浓度高达 32μg/mL 不会显著影响秀丽隐杆线虫的存活;然而,浓度等于或高于该值会以剂量依赖的方式显著影响线虫的存活。

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