Design, Synthesis, and Antibacterial Evaluation of Novel Ocotillol Derivatives and Their Synergistic Effects with Conventional Antibiotics.
Design, Synthesis, and Antibacterial Evaluation of Novel Ocotillol Derivatives and Their Synergistic Effects with Conventional Antibiotics.
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新型奥克替醇衍生物的设计、合成、抗菌评价及其与常规抗生素的协同作用
DOI：
10.3390/molecules26195969
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发表时间：
2021-10-01
期刊：
影响因子：
--
通讯作者：
Bi Y
中科院分区：
文献类型：
--
作者：
Zhang D;Cao Y;Wang K;Shi Z;Wang R;Meng Q;Bi Y
抗生素使用不当导致细菌产生耐药性，导致许多细菌感染的抗生素减少。尤其是医院获得性耐甲氧西林金黄色葡萄球菌(HA-MRSA)的耐药性尤为严重。本研究设计并合成了两个系列的3-取代奥克替醇衍生物，以提高其抗HA-MRSA的效力和协同抗菌活性。在合成的化合物中，20-31 种在体外对 HA-MRSA 18-19、18-20 和金黄色葡萄球菌 ATCC29213 的最低抑制浓度 (MIC) 值为 1-64 µg/mL。化合物21的抗菌活性最好，MIC为1μg/mL，具有协同抑制作用。当与氯霉素（CHL）或卡那霉素（KAN）组合时，分数抑制浓度指数（FICI）值为0.375。还总结了奥克替洛尔型衍生物的构效关系（SAR）。化合物21有潜力被开发为新型抗菌剂或针对HA-MRSA的增强剂。
The improper use of antibiotics has led to the development of bacterial resistance, resulting in fewer antibiotics for many bacterial infections. Especially, the drug resistance of hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA) is distinctly serious. This research designed and synthesized two series of 3-substituted ocotillol derivatives in order to improve their anti-HA-MRSA potency and synergistic antibacterial activity. Among the synthesized compounds, 20–31 showed minimum inhibitory concentration (MIC) values of 1–64 µg/mL in vitro against HA-MRSA 18–19, 18–20, and S. aureus ATCC29213. Compound 21 showed the best antibacterial activity, with an MIC of 1 μg/mL and had synergistic inhibitory effects. The fractional inhibitory concentration index (FICI) value was 0.375, when combined with chloramphenicol (CHL) or kanamycin (KAN). The structure–activity relationships (SARs) of ocotillol-type derivatives were also summarized. Compound 21 has the potential to be developed as a novel antibacterial agent or potentiator against HA-MRSA.
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影响因子：
3.8
作者：
Oloyede, H. O. B.;Ajiboye, H. O.;Ajiboye, T. O.
通讯作者：
Ajiboye, T. O.
影响因子：
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作者：
Kim JH;Yi YS;Kim MY;Cho JY
通讯作者：
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影响因子：
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作者：
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影响因子：
1.8
作者：
Lin, Geng-Jie;Luo, Shi-Peng;Huang, Pei-Qiang
通讯作者：
Huang, Pei-Qiang
影响因子：
3
作者：
Bi, Yi;Ma, Cong;Xu, Jinyi
通讯作者：
Xu, Jinyi