耐甲氧西林金黄色葡萄球菌（MRSA）丙酮酸激酶的新型抑制剂
Novel inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase.
作者信息
El-Sayed Mardia Telep, Zoraghi Roya, Reiner Neil, Suzen Sibel, Ohlsen Knut, Lalk Michael, Altanlar Nurten, Hilgeroth Andreas
机构信息
a Department of Pharmaceutical Chemistry , Institute of Pharmacy, Martin Luther University , Halle , Germany .
b Department of Medicine, Division of Infectious Diseases , University of British Columbia , Vancouver , BC , Canada .
出版信息
J Enzyme Inhib Med Chem. 2016 Dec;31(6):1666-71. doi: 10.3109/14756366.2015.1118685. Epub 2015 Dec 10.
Novel bisindolyl-cycloalkane indoles resulted from the reaction of aliphatic dialdehydes and indole. As bisindolyl-natural alkaloid compounds have recently been reported as inhibitors of the methicillin-resistant Staphylococcus aureus (MRSA)-pyruvate kinase (PK), we tested our novel compounds as MRSA PK inhibitors and now report first inhibiting activities. We discuss structure-activity relationships of structurally varied compounds. Activity influencing substituents have been characterized and relations to antibacterial activities of the most active compounds have been proved.
新型双吲哚基环烷烃吲哚是脂肪族二醛与吲哚反应的产物。由于最近有报道称双吲哚基天然生物碱化合物是耐甲氧西林金黄色葡萄球菌（MRSA）丙酮酸激酶（PK）的抑制剂，我们将我们的新型化合物作为MRSA PK抑制剂进行了测试，现在报告其首次抑制活性。我们讨论了结构各异的化合物的构效关系。已对影响活性的取代基进行了表征，并证明了其与活性最高的化合物的抗菌活性之间的关系。
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