Evaluation of antimicrobial activity of synthesized 9H-alkylcarbazole and 10H-alkylphenothiazine derivatives on the cells of Salmonella enterica ser. Typhimurium, Saccharomyces cerevisiae, and Candida albicans

S. Sutkuvienė, S. Sakalauskaite, Neringa Kuliešienė, L. Ragelienė, R. Daugelavičius
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Abstract

2 Department of Biochemistry, Faculty of Medicine, Lithuanian University of Health Sciences, Tilžės str. 18, 47181 Kaunas, Lithuania 10H-substituted phenothiazine and 9H-substituted carbazole derivatives are important because of a very wide range of applications and especially in medical chemistry due to their pharmacological activities. In this study, we synthesized 9H-alkylcarbazole and 10H-alkylphenothiazine derivatives with various lengths of alkyl chains and evaluated their antimicrobial and efflux inhibiting activities on the cells of Salmonella enterica ser. Typhimurium, Saccharomyces cerevisiae, and Candida albicans. Results of our study revealed that an increased length of alkyl chains of the carbazoles increased the accumulation of efflux indicator tetraphenylphosphonium (TPP+) ions. Cells of S. enterica efflux mutant ΔTolC had a considerable susceptibility to the synthesized compounds. The compounds exerted synergy with fluconazole against S. cerevisiae yeast. Efflux pump mutant ΔPdr5 was hypersensitive to the investigated carbazole and phenothiazine derivatives. The inhibitory effect of the compounds with a shorter alkyl chain (10-methyl-10H-phenothiazine and 9-methyl-9H-carbazole) was the highest for Candida albicans cells.
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合成的9h -烷基咔唑和10h -烷基吩噻嗪衍生物对肠道沙门氏菌细胞的抑菌活性评价。鼠伤寒菌,酿酒酵母菌和白色念珠菌
2立陶宛卫生科学大学医学院生物化学系,Tilžės str. 18, 47181立陶宛Kaunas, 10h -取代吩噻嗪和9h -取代咔唑衍生物具有非常广泛的应用,特别是由于其药理活性而在医学化学中具有重要意义。在本研究中,我们合成了不同长度烷基链的9h -烷基咔唑和10h -烷基吩噻嗪衍生物,并评价了它们对肠沙门氏菌细胞的抗菌和外排抑制活性。鼠伤寒菌,酿酒酵母菌和白色念珠菌。我们的研究结果表明,随着咔唑烷基链长度的增加,外排指示剂四苯基磷(TPP+)离子的积累增加。肠链球菌外排突变体ΔTolC的细胞对合成的化合物有相当大的敏感性。这些化合物与氟康唑对酿酒酵母具有协同作用。外排泵突变体ΔPdr5对所研究的咔唑和吩噻嗪衍生物过敏。烷基链较短的化合物(10-甲基- 10h -吩噻嗪和9-甲基- 9h -咔唑)对白色念珠菌细胞的抑制作用最高。
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