Synthesis and biological activity of 2,5-dimethyltetrahydrothiopyran-4-one mono- and diacetylenic derivatives

2014

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DOI 10.1055/s-0034-1382636
Data confidence 70 medium
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Abstract

Mono- and diacetylenic alcohols and glycols of the tetrahydrothiopyran row were synthesized by Favorskii reaction. Steric structures of the compounds were established by NMR ( 1 H and 13 C) and Mass spectra. The antibacterial, antifungal and antileishmanial activities of the compounds were screened. Compounds 1, 6 and 7 were found to be more active than others against Staphylococcus aureus (IC 50 = 10.05, 1.38, 10.28 µg/mL) and Methicillin-resistant Staphylococcus aureus (IC 50 = 18.2, 1.14, 12.85 µg/mL), respectively. Only compound 6 showed good activity against Mycobacterium intracellulare with IC 50 value equal 2.54 µg/mL. Fig. 1