Li Wei, Sanchez-Hidalgo Andrea, Jones Victoria, de Moura Vinicius Calado Nogueira, North E Jeffrey, Jackson Mary
Mycobacteria Research Laboratories, Department of Microbiology, Immunology and Pathology, Colorado State University, Fort Collins, Colorado, USA.
Creighton University, School of Pharmacy & Health Professions, Department of Pharmacy Sciences, Omaha, Nebraska, USA.
Antimicrob Agents Chemother. 2017 Mar 24;61(4). doi: 10.1128/AAC.02399-16. Print 2017 Apr.
A number of inhibitors of the essential mycolic acid transporter, MmpL3, are currently under development as potential novel antituberculosis agents. Using the checkerboard method to study the interaction profiles of various antituberculosis drugs or experimental compounds with two different chemotypes inhibiting this transporter (indolcarboxamides and adamantyl ureas), we showed that MmpL3 inhibitors act synergistically with rifampin, bedaquiline, clofazimine, and β-lactams.
作为潜在的新型抗结核药物,多种必需分枝菌酸转运蛋白MmpL3的抑制剂目前正在研发中。我们使用棋盘法研究了各种抗结核药物或实验化合物与抑制该转运蛋白的两种不同化学类型(吲哚羧酰胺和金刚烷基脲)的相互作用情况,结果表明MmpL3抑制剂与利福平、贝达喹啉、氯法齐明和β-内酰胺类药物具有协同作用。