Synthesis of the novel cage amides and imides and evaluation of their antibacterial and antifungal activity

V. Palchykov, A. Gaponov, N. Manko, N. Finiuk, О. Novikevych, O. Gromyko, R. Stoika, N. Pokhodylo
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Abstract

Cage amides and imides bearing bicyclo[2.2.1]- and bicyclo[2.2.2]-subunits were synthesized and evaluated both for antimicrobial activity toward five key ESKAPE pathogenic bacteria: one Gram‐positive bacteria methicillin‐resistant Staphylococcus aureus (ATCC 43300), four Gram‐negative bacteria Escherichia coli (ATCC 25922), Klebsiella pneumoniae (ATCC 700603), Acinetobacter baumannii (ATCC 19606) and Pseudomonas aeruginosa (ATCC 27853) and for antifungal activity towards pathogenic fungal strains Candida albicans (ATCC 90028) and Cryptococcus neoformans var. Grubii (H99; ATCC 208821). Compound VP-4539 with bicyclo[2.2.2]octene motif demonstrated the highest cytotoxic activity towards C. neoformans, while human keratinocytes of HaCaT line, murine fibroblasts of Balb/c 3T3 line and mitogen-activated lymphocytes of peripheral human blood were found to be tolerant to its action. VP-4539 compound did not intercalate into salmon sperm DNA indicating that its cytotoxicity is not related to intercalation into nucleic acid. Keywords: antifungal, antimicrobial, bicyclo[2.2.1]heptane, bicyclo[2.2.2]octene, cytotoxicity, DNA intercalation, human keratinocytes, lymphocytes, сage compounds
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新型笼状酰胺和亚胺的合成及其抗菌和抗真菌活性的评价
合成了含有双环[2.2.1]-和双环[2.2.2]-亚基的笼状酰胺和亚胺,并对5种主要ESKAPE致病菌进行了抑菌活性评价:1种革兰氏阳性细菌耐甲氧西林金黄色葡萄球菌(ATCC 43300)、4种革兰氏阴性细菌大肠杆菌(ATCC 25922)、肺炎克雷伯菌(ATCC 700603)、鲍曼不动杆菌(ATCC 19606)和铜绿假单胞菌(ATCC 27853),以及对致病性真菌菌株白色念珠菌(ATCC 90028)和新型隐球菌var. Grubii (H99;写明ATCC 208821)。含有双环[2.2.2]辛烯基序的化合物VP-4539对新生c具有最高的细胞毒活性,而HaCaT系人角质形成细胞、Balb/c 3T3系小鼠成纤维细胞和人外周血有丝分裂原活化淋巴细胞对其具有耐受性。VP-4539化合物未嵌入鲑鱼精子DNA,表明其细胞毒性与嵌入核酸无关。关键词:抗真菌,抗菌,双环[2.2.1]庚烷,双环[2.2.2]辛烯,细胞毒性,DNA嵌入,人角质形成细胞,淋巴细胞,脂肪化合物
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