Hetaryl- and heteroarylvinyl-substituted nitrofurans identified as non-cytotoxic selective antitubercular agents |
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Affiliation: | 1. Institute of Chemistry, St. Petersburg State University, 199034 St. Petersburg, Russian Federation;2. Pharmaceutical Technology Transfer Center, K. D. Ushinsky Yaroslavl State Pedagogical University, 150000 Yaroslavl, Russian Federation;3. St. Petersburg Research Institute of Phthisiopulmonology, 191036 St. Petersburg, Russian Federation |
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Abstract: | New (E)-5-[2-(5-nitrofuran-2-yl)vinyl]-1,2,4-oxadiazoles and 5-(5-nitrofuran-2-yl)-1,2,4-oxadiazoles were synthesized via the base-promoted condensation of nitrofuran-containing acyl chlorides with amidoximes. Testing these compounds against Gram-negative E. coli, Gram-positive B. subtilis and S. aureus as well as M. tuberculosis HRv37 strain revealed three compounds being selectively antimycobacterial. None of these compounds displayed any cytotoxicity towards human pancreatic epithelioid carcinoma cell line, PANC-1. |
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Keywords: | nitrofurans 124-oxadiazoles amidoximes olefin linker direct bond antibacterial assay antimycobacterial assay MTT assay cell viability |
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