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Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold |
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| Authors: | Violina T Angelova Violeta Valcheva Nikolay G Vassilev Rosen Buyukliev Georgi Momekov Ivan Dimitrov Luciano Saso Mirjana Djukic Boris Shivachev |
| Institution: | 1. Department of Chemistry, Faculty of Pharmacy, Medical University of Sofia, 2, Dunav St., 1000 Sofia, Bulgaria;2. Institute of Microbiology, Bulgarian Academy of Sciences, 26, Acad. G. Bonchev St., 1113 Sofia, Bulgaria;3. Laboratory of Nuclear Magnetic Resonance, Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, 9, Acad. G. Bonchev St., 1113 Sofia, Bulgaria;4. Laboratory of Experimental Chemotherapy, Department of Pharmacology, Pharmacotherapy and Toxicology, Faculty of Pharmacy, Medical University-Sofia, 2, Dunav St., 1000 Sofia, Bulgaria;5. Department of Physiology and Pharmacology “Vittorio Erspamer”, Sapienza University, P.le Aldo Moro 5, 00185 Rome, Italy;6. Department for Toxicology, Faculty of Pharmacy, University of Belgrade, 450, Vojvode Stepe, St., 11221 Belgrade, Serbia;7. Bulgarian Academy of Sciences, Institute of Mineralogy and Crystallography, 107, Acad. G. Bonchev St., 1113 Sofia, Bulgaria |
| Abstract: | This study reports the synthesis of new 2H-chromene or coumarin based acylhydrazones, which were evaluated for their in vitro antimycobacterial activity against reference strain Mycobacterium tuberculosis H37Rv and compared to the first-line antituberculosis drugs, isoniazid (INH) and ethambutol (EMB). The most active compounds 7m (MIC 0.13 μM), 7o (MIC 0.15 μM) and 7k (MIC 0.17 μM) demonstrated antimycobacterial activity at submicromolar concentration level and remarkably minimal associated cytotoxicity in the human embryonic kidney cell line HEK-293T. Structure-activity relationship for this class of compounds has been established. |
| Keywords: | Antitmycobacterial activity Coumarin Cytotoxicity Hydrazide-hydrazone |
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