一种经过改良的恶唑烷酮，对结核分枝杆菌和革兰氏阳性菌具有选择性效力。
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
作者信息
Kaushik Amit, Heuer Abigail M, Bell Drew T, Culhane Jeffrey C, Ebner David C, Parrish Nicole, Ippoliti J Thomas, Lamichhane Gyanu
机构信息
Taskforce to Study Resistance Emergence & Antimicrobial Development Technology and Center for Tuberculosis Research, Department of Medicine, Johns Hopkins University, 1550 Orleans St, Baltimore, MD 21287, United States.
Department of Chemistry, University of St. Thomas, St. Paul, MN 55105, United States.
出版信息
Bioorg Med Chem Lett. 2016 Aug 1;26(15):3572-6. doi: 10.1016/j.bmcl.2016.06.019. Epub 2016 Jun 9.
Innovation of new antibacterials that are effective against strains that have developed resistance to existing drugs would strengthen our ability to treat and subsequently control spread of pathogenic bacteria. Increasing incidence of infections with drug resistant bacteria has become a common occurrence in recent times. We have developed an evolved oxazolidinone, T145, which inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. The oxazolidinone is bactericidal against Mtb but bacteriostatic against E. faecalis and S. aureus. In addition to therapeutically valuable potency and bactericidal activity against Mtb, T145 minimizes selection of spontaneous resistant mutants, a trait that prolongs longevity of a drug in clinical use.
研发出对已对现有药物产生耐药性的菌株有效的新型抗菌药物，将增强我们治疗并进而控制病原菌传播的能力。近年来，耐药菌感染发病率不断上升已成为常见现象。我们研发了一种经过改良的恶唑烷酮T145，它对粪肠球菌、金黄色葡萄球菌和结核分枝杆菌（Mtb）具有抑制生长的作用，其亚微克/毫升的效力具有潜在的治疗价值。该恶唑烷酮对结核分枝杆菌具有杀菌作用，但对粪肠球菌和金黄色葡萄球菌具有抑菌作用。除了具有治疗价值的效力和对结核分枝杆菌的杀菌活性外，T145还能将自发耐药突变体的选择降至最低，这一特性可延长药物在临床使用中的寿命。
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