Cao Yucheng, Wang Kaiyi, Wang Jiali, Cheng Haoran, Ma Mengxin, Meng Qingguo, Li Xiaopeng, Bi Yi
School of Pharmacy, Key Laboratory of Molecular Pharmacology & Drug Evaluation, Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System & Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, PR.
Future Med Chem. 2021 Jun;13(12):1025-1039. doi: 10.4155/fmc-2020-0364. Epub 2021 Apr 30.
With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant (HA-MRSA), novel derivatives of ocotillol were synthesized. Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for antibacterial activity. Compounds exhibited potent antibacterial activity against HA-MRSA, with MIC = 8-64 μg/ml. Additionally, a combination of compound and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Compound has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.
随着抗菌药物的滥用日益严重，多重耐药菌已成为人类健康和医疗系统的负担。为了找到对医院获得性耐甲氧西林金黄色葡萄球菌（HA-MRSA）有效的替代化合物，合成了新的奥科梯隆衍生物。合成了含多环氮基团的奥科梯隆衍生物，并对其抗菌活性进行了评估。这些化合物对HA-MRSA表现出强效抗菌活性，最低抑菌浓度（MIC）为8 - 64μg/ml。此外，该化合物与市售抗生素卡那霉素的组合显示出协同抑制作用，分级抑菌浓度指数≤0.375。该化合物具有很强的抑制作用，这种衍生物有潜力作为探索抗菌机制的药理学工具。
