Considering the promising antimicrobial activity of compounds bearing the thiazole or the oxadiazole rings in their structures, we set out to obtain new antimicrobial molecules bearing the 2-(thiazol-5-yl)-1,3,4-oxadiazole schaffold. The structures of the 8 new compounds obtained was confirmed by physicochemical characterization including: 1H-NMR, MS and elemental analysis. Antimicrobial activity was investigated against 5 Gram-positive bacterial strains, 2 Gram-negative bacterial strains and 2 fungal strains. The newly synthesized compounds showed modest antimicrobial activity.
Considering the well-established antifungal activity of azole compounds, a new series of thiazolyl-methylen-1,3,4-oxadiazolines derivatives were designed and synthesized as lanosterol-demethylase inhibitors. The final compounds were screened for antifungal activity against the Candida albicans ATCC 90028 strain. Molecular docking studies were performed to investigate the interaction modes between the compounds and the active site of lanosterol 14a-demethylase, which is a target enzyme for anticandidal azoles. Theoretical ADME predictions were also calculated for the final compounds 5a-h.
In an effort to obtain new NSAIDs, that act as COX-2 selective inhibitors with simultaneous iNOS inhibition properties and direct antioxidant activity, we designed a series of 8 new compounds bearing the 5-thiazolyl-carbohydrazon-N-allyl-thiazoline scaffold. The synthesized compounds were physicochemically characterized by: 1H-NMR, MS and elemental analysis. An initial, in vitro, free radical scavenging assay (DPPH bleaching) test showed that most compounds are superior to standard antioxidants Trolox and BHT.
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