Department of Microbiology & Immunology, School of Medicine, Soonchunhyang University, Cheonan, Chungnam 31151, South Korea.
Department of Life Science & Biotechnology, Soonchunhyang University, Asan, Chungnam 31538, South Korea.
Future Med Chem. 2021 Feb;13(3):251-267. doi: 10.4155/fmc-2019-0154. Epub 2020 Dec 9.
Tuberculosis is the leading cause of mortality among infectious diseases worldwide. Finding a new competent anti tubercular therapy is essential. We screened thousands of compounds and evaluated their efficacy against . Initially, 2-nitronaphtho[2,3-b]benzofuran-6,11-dione was active against . Next, among 15 newly synthesized derivatives, BNF15 showed promising effect against all drug-sensitive and drug-resistant (MIC: 0.02-0.78 μg/ml). BNF15 effectively killed intracellular and nontuberculous mycobacteria. BNF15 exhibited a prolonged post antibiotic effect superior to isoniazid, streptomycin, and ethambutol and synergistic interaction with rifampicin. In acute oral toxicity test, BNF15 did not show toxic effect at a concentration up to 2000 mg/kg. These results highlight the perspective of BNF15 to treat drug-resistant .
结核病是全球传染病死亡的主要原因。寻找新的有效的抗结核治疗方法至关重要。我们筛选了数千种化合物，并评估了它们对的疗效。最初，2-硝基萘并[2,3-b]苯并呋喃-6,11-二酮对具有活性。接下来，在 15 种新合成的衍生物中，BNF15 对所有药敏和耐药（MIC：0.02-0.78μg/ml）均显示出良好的效果。BNF15 能有效杀灭细胞内和非结核分枝杆菌。BNF15 表现出优于异烟肼、链霉素和乙胺丁醇的延长抗生素后效应，并与利福平具有协同作用。在急性口服毒性试验中，BNF15 在高达 2000mg/kg 的浓度下没有显示出毒性作用。这些结果突出了 BNF15 治疗耐药的潜力。
