耐甲氧西林金黄色葡萄球菌 (MRSA) 丙酮酸激酶 (PK) 抑制剂及其抗菌活性。
Methicillin-Resistant Staphylococcus Aureus (MRSA) Pyruvate Kinase (PK) Inhibitors and their Antimicrobial Activities.
机构信息
Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu, Sichuan 610041, China.
出版信息
Curr Med Chem. 2022;29(5):908-923. doi: 10.2174/0929867328666210322103340.
Resistance to antibiotics has existed in the health care and community settings. Thus, developing novel antibiotics is urgent. Methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase (PK) is crucial for the survival of bacteria, making it a novel antimicrobial target. In the past decade, the most commonly reported PK inhibitors include indole, flavonoid, phenazine derivatives from natural products' small molecules or their analogs, or virtual screening from small molecule compound library. This review covers the PK inhibitors and their antimicrobial activities reported from the beginning of 2011 through mid-2020. The Structure-Activity Relationships (SARs) were discussed briefly as well.
抗生素耐药性在医疗保健和社区环境中一直存在。因此，开发新型抗生素迫在眉睫。耐甲氧西林金黄色葡萄球菌 (MRSA) 丙酮酸激酶 (PK) 对细菌的生存至关重要，使其成为一种新型抗菌药物靶标。在过去的十年中，报道最多的 PK 抑制剂包括天然产物小分子中的吲哚、类黄酮、吩嗪衍生物或其类似物，或从小分子化合物库中进行虚拟筛选。本综述涵盖了 2011 年初至 2020 年年中报道的 PK 抑制剂及其抗菌活性。还简要讨论了构效关系 (SAR)。
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