Yang Baowei, Mei Yicheng, Li Qianhui, Zhang Mengyuan, Tang Huiling, Liu Tong, Feng Feng, Fu Qiyun, Jiang Yuzhang, Ye Qizhuang
School of Pharmacy, Jiangsu Food & Pharmaceutical Science College, Huai'an, Jiangsu, 223003, China.
Department of Laboratory, Huai'an First People's Hospital, Nanjing Medical University, Huai'an, Jiangsu, 223300, China.
Future Med Chem. 2021 Jun;13(11):959-974. doi: 10.4155/fmc-2021-0030. Epub 2021 Mar 30.
There is an urgent need for new antibiotics and alternative strategies to combat bacterial pathogens. Molecular docking, antibacterial evaluation and , cytotoxicity assessment and enzyme inhibition analyses were performed. Compound exhibited antimicrobial activity against (MIC: 4 μg/ml), various clinically isolated strains of MRSA (MIC: 4-16 μg/ml) and (MIC: 4 μg/ml) when combined with subinhibitory concentrations of colistin B. Compound (20 mg/kg) yielded mild improvement in survival of methicillin-resistant (MRSA)-infected mice. Additionally, enzyme inhibition tests showed that compound exhibited inhibitory effects against dihydrofolate reductase (105.1 μg/ml) and DNA gyrase (122.8 μg/ml). Compound is a promising antibacterial candidate for further development.
迫切需要新的抗生素和替代策略来对抗细菌病原体。进行了分子对接、抗菌评估、细胞毒性评估和酶抑制分析。化合物与亚抑制浓度的多粘菌素B联合使用时，对肺炎克雷伯菌（MIC：4μg/ml）、各种临床分离的耐甲氧西林金黄色葡萄球菌菌株（MIC：4 - 16μg/ml）和鲍曼不动杆菌（MIC：4μg/ml）表现出抗菌活性。化合物（20mg/kg）使耐甲氧西林金黄色葡萄球菌（MRSA）感染小鼠的存活率有轻微提高。此外，酶抑制试验表明化合物对二氢叶酸还原酶（105.1μg/ml）和DNA促旋酶（122.8μg/ml）具有抑制作用。化合物是一种有前景的抗菌候选物，有待进一步开发。
