Discovery of novel hydantoin and thiazolidindione derivatives as antimycobacterial agents

Discovery of novel hydantoin and thiazolidindione derivatives as antimycobacterial agents

Poster

Nadezhda Yanakieva1, Rossen Buyukliev1, Violeta Valcheva2, Violina Angelova1
1Faculty of Pharmacy, Medical University of Sofia, Sofia, Bulgaria
2”Stefan Angelov” Institute of Microbiology, Bulgarian Academy of Sciences, Sofia, Bulgaria

A series of new hydantoin and thiazolidindione derivatives were synthesized by a Knoevenagel condensation. The compounds were identified by their melting points, 1H NMR, 13C NMR, and HR-MS spectral data. In vitro antimycobacterial activity was evaluated against reference strain Mycobacterium tuberculosis H37Rv and compared to that of the first-line antituberculosis drugs isoniazid (INH) and ethambutol (EMB). The new compounds show promising antimycobacterial activity (MIC ranging from 0.7505 to 1.5475 µM) and low cytotoxicity in the human embryonic kidney cell line HEK-293T (IC50 > 200 µM). The most potent compound in the series 3a, could be a promising drug candidate for further development.
Key words: antimycobacterial activity, hydantoin, thiazolidine-2,4-dione