Antimycobacterial activity of novel hydrazide-hydrazone derivatives with 2H-chromene and coumarin scaffold
- Angelova, V. T.
- Valcheva, V.
- Vassilev, N. G.
- Buyukliev, R.
- Momekov, G.
- Dimitrov, I.
- Saso, L.
- Djukic, M.
- Shivachev, B.
Publication date
January 2017
DOI Publisher
Elsevier BV ISSN
0960-894X Citation count (estimate)
6Abstract
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 mu M), 7o (MIC 0.15 mu M) and 7k (MIC 0.17 mu M) 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. (C) 2016 Elsevier Ltd. All rights reserved
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