Lubenets Vira, Vasylyuk Sofiya, Monka Nataliya, Bolibrukh Khrystyna, Komarovska-Porokhnyavets Olena, Baranovych Diana, Musyanovych Rostyslav, Zaczynska Ewa, Czarny Anna, Nawrot Urszula, Novikov Volodymyr
Department of Technology of Biologically Active Substances, Pharmacy & Biotechnology, Lviv National Polytechnic University, S. Bandery Str. 12, Lviv, Ukraine.
Institute of Immunology & Experimental Therapy, Polish Academy of Sciences, R. Weigla Str. 12, 53-114 Wrocław, Poland.
Saudi Pharm J. 2017 Feb;25(2):266-274. doi: 10.1016/j.jsps.2016.06.007. Epub 2016 Jul 1.
A series of esters of 4-acetyl, 4-trifluoroacetyl- and 4-(3-chloropropionyl)aminobenzenethiosulfoacids (twenty-four compounds) were synthesized and characterized by elemental analysis, H NMR and IR spectroscopy. The antibacterial activity of the novel candidates has been screened using the agar diffusion or serial dilution methods against representative Gram-positive (, , , sp., ), Gram-negative ( sp., , , , , ) bacteria and fungi (, , , , , , , ). Particular potency has been discovered against all tested pathogenic bacteria and fungi by compounds and at nanomolar concentrations. Some appropriate effect of thiosulfoesters structure upon their antimicrobial activity was determined.
合成了一系列4-乙酰基、4-三氟乙酰基和4-(3-氯丙酰基)氨基苯硫代磺酸酯（共24种化合物），并通过元素分析、核磁共振氢谱和红外光谱对其进行了表征。采用琼脂扩散法或系列稀释法，针对代表性革兰氏阳性菌（金黄色葡萄球菌、表皮葡萄球菌、枯草芽孢杆菌、粪肠球菌、屎肠球菌）、革兰氏阴性菌（大肠杆菌、肺炎克雷伯菌、阴沟肠杆菌、铜绿假单胞菌、鲍曼不动杆菌）和真菌（白色念珠菌、热带念珠菌、近平滑念珠菌、光滑念珠菌、克柔念珠菌、新型隐球菌、烟曲霉、黄曲霉）对这些新型化合物的抗菌活性进行了筛选。化合物1和2在纳摩尔浓度下对所有测试的病原菌和真菌均表现出特别强的效力。确定了硫代磺酸酯结构对其抗菌活性的一些适当影响。
