Hafij Al Mahmud1, Hoonhee Seo1, Sukyung Kim1, Md Imtiazul Islam1, Omme Fatema Sultana1, Kung-Woo Nam2, Byung-Eui Lee3, Venkata S Sadu4, Kee-In Lee4,5, Ho-Yeon Song1. 1. Department of Microbiology & Immunology, School of Medicine, Soonchunhyang University, Cheonan, Chungnam 31151, South Korea. 2. Department of Life Science & Biotechnology, Soonchunhyang University, Asan, Chungnam 31538, South Korea. 3. Department of Chemistry, School of Life Sciences, Soonchunhyang University, Asan, Chungnam 31538, South Korea. 4. Major of Green Chemistry & Environmental Biotechnology, University of Science & Technology, Daejeon 34113, South Korea. 5. Green Chemistry Division, Korea Research Institute of Chemical Technology, Daejeon 34114, South Korea.
Abstract
Aim: Tuberculosis is the leading cause of mortality among infectious diseases worldwide. Finding a new competent anti tubercular therapy is essential. Materials & methods: We screened thousands of compounds and evaluated their efficacy against Mycobacterium tuberculosis. Results: Initially, 2-nitronaphtho[2,3-b]benzofuran-6,11-dione was active against M. tuberculosis. Next, among 15 newly synthesized derivatives, BNF15 showed promising effect against all drug-sensitive and drug-resistant M. tuberculosis (MIC: 0.02-0.78 μg/ml). BNF15 effectively killed intracellular M. tuberculosis 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. Conclusion: These results highlight the perspective of BNF15 to treat drug-resistant M. tuberculosis.
Aim: Tuberculosis is the leading cause of mortality among infectious diseases worldwide. Finding a new competent anti tubercular therapy is essential. Materials & methods: We screened thousands of compounds and evaluated their efficacy against Mycobacterium tuberculosis. Results: Initially, 2-nitronaphtho[2,3-b]benzofuran-6,11-dione was active against M. tuberculosis. Next, among 15 newly synthesized derivatives, BNF15 showed promising effect against all drug-sensitive and drug-resistant M. tuberculosis (MIC: 0.02-0.78 μg/ml). BNF15 effectively killed intracellular M. tuberculosis 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. Conclusion: These results highlight the perspective of BNF15 to treat drug-resistant M. tuberculosis.
Entities:
Keywords:
BNF15; PAE; acute oral toxicity; drug combination; drug-resistant M. tuberculosis
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