Solecka Jolanta, Rajnisz Aleksandra, Postek Magdalena, Laudy Aginieszka E, Szawkalo Joanna, Czarnocki Zbigniew
Acta Pol Pharm. 2016 Sep;73(5):1181-1189.
This study is a continuation of a research program aimed at identifying potent drugs against bacterial infections, in which a series of organic compounds: dicarboxylic acid imides and thioimides, isoquinoline derivatives and open chain compounds, were examined for antimicrobial properties against Staphylococcus auneus and Escheiichia coli. In effect of this investigation, the most active compounds (35-40, 47) were selected for in vitiv tests against fourteen clinically important pathogenic isolates, the methicillin resistant Staphylococcus aueus (MRSA) and several reference Gram-negative bacteria: Prteus vulgaris, Pseudomonas aeruginosa, Klebsiella pneumonia, Stenonophoinonas inaltophilia, and Acinetobacter baumannii. The obtained data revealed that seven compounds (three dithioimides, 35, 39, 47, and four thioimides, 36-38, 40) exhibit effective antibacterial activity against the tested Staphylococcus auirus MSSA and MRSA strains. Among them, dicarboxylic acid thioimides 37 and 38 were proven to be the most active.
本研究是一项旨在鉴定抗细菌感染强效药物的研究计划的延续，该计划中检测了一系列有机化合物：二羧酸酰亚胺和硫代酰亚胺、异喹啉衍生物及开链化合物对金黄色葡萄球菌和大肠杆菌的抗菌特性。通过这项研究，选择了最具活性的化合物（35 - 40、47）针对14种临床上重要的致病分离株、耐甲氧西林金黄色葡萄球菌（MRSA）以及几种革兰氏阴性参考菌：普通变形杆菌、铜绿假单胞菌、肺炎克雷伯菌、嗜麦芽窄食单胞菌和鲍曼不动杆菌进行体外测试。所得数据表明，七种化合物（三种二硫代酰亚胺，35、39、47，以及四种硫代酰亚胺，36 - 38、40）对测试的金黄色葡萄球菌MSSA和MRSA菌株表现出有效的抗菌活性。其中，二羧酸硫代酰亚胺37和38被证明活性最强。
