Department of Pharmaceutical Microbiology and Parasitology, Faculty of Pharmacy, Medical University of Silesian Piasts in Wroclaw, Borowska 211, 50-556 Wroclaw, Poland.
Department of Medicinal Chemistry, Faculty of Pharmacy, Medical University of Silesian Piasts in Wroclaw, Borowska 211, 50-556 Wroclaw, Poland.
Molecules. 2020 Jul 31;25(15):3503. doi: 10.3390/molecules25153503.
The global concern related with growing number of bacterial pathogens, resistant to numerous antibiotics, prone scientific environment to search for new antimicrobials. Antiseptics appear to be suitable candidates as adjunctive agents to antibiotics or alternative local treatment option aiming to prevent and treat infections. 1,2-benzothiazines are considered one the most promising of them. In this research twenty 1,2-benzothiazine 1,1-dioxide derivatives were scrutinized with regard to their biological activity. Three of them are new. For evaluation of compounds' activity against microbial pathogens, disk diffusion method and serial microdilution method was applied. To establish the cytotoxicity profile of tested 1,2-benzothiazines 1,1-dioxides derivatives, the cytotoxicity assay using fibroblasts L292 was performed. Antimicrobial activity of all tested compounds against Gram-positive and strains was higher than antimicrobial activity of DMSO solvent, which possesses antimicrobial activity itself. Gram-negative , and have shown susceptibility only to compounds , and . None of tested compounds was effective against Compound has demonstrated the strongest antimicrobial potency (MIC = 0.00975 mg/mL) among compounds of series . Compounds of series , namely , , had the lowest minimum inhibitory concentration (MIC). Compound displayed also the lowest cytotoxic effect against fibroblast cell line among series compounds. All tested derivatives displayed lower MIC against Gram-positive bacteria than commercially applied antiseptic, povidone iodine, which MIC value range for tested Gram-positive bacteria was 1.56-6.25 mg/mL.
全球范围内，细菌病原体的数量不断增加，且对多种抗生素具有耐药性，这种情况促使科学界寻找新的抗菌药物。防腐剂作为抗生素的辅助剂或替代局部治疗选择，似乎是合适的候选药物，旨在预防和治疗感染。1,2-苯并噻嗪类化合物被认为是最有前途的抗菌药物之一。在这项研究中，对二十种 1,2-苯并噻嗪 1,1-二氧化物衍生物进行了生物活性研究。其中三种是新的。为了评估化合物对微生物病原体的活性，采用了圆盘扩散法和连续微量稀释法。为了建立测试的 1,2-苯并噻嗪 1,1-二氧化物衍生物的细胞毒性谱，使用成纤维细胞 L292 进行了细胞毒性测定。所有测试化合物对革兰氏阳性菌和革兰氏阴性菌的抗菌活性均高于 DMSO 溶剂的抗菌活性，而 DMSO 溶剂本身也具有抗菌活性。革兰氏阴性菌 、 和 仅对化合物 、 和 敏感。测试的化合物对 均无效。化合物 表现出最强的抗菌效力（MIC = 0.00975 mg/mL），在系列化合物中。化合物系列 、 、 具有最低的最小抑菌浓度（MIC）。化合物 对成纤维细胞系的细胞毒性也最低。所有测试的衍生物对革兰氏阳性菌的 MIC 均低于市售防腐剂聚维酮碘，聚维酮碘对测试的革兰氏阳性菌的 MIC 值范围为 1.56-6.25 mg/mL。
