Following the principle of union of active group, the thiochromanone was combined with 1,3,4-oxadiazole, and 12 compounds were designed and synthesized. The target compounds were confirmed by 1 H NMR and HRMS. The preliminary antifungal activity assay showed that most of the target compounds exhibited significant inhibition activity against four animal pathogenic fungi and four plant pathogenic fungi. Among them, the minimum inhibitory concentration (MIC) value of compound 4f against Canidia albicans reached 4 μg•mL -1 , and the MIC value of 4d against Aspergillusnigervan tiegh reached 8 μg•mL -1 , which were higher than the positive controls. And the molecular docking studies have found that 4f has strong binding ability to CYP51 of Canidia albicans, which may be a potential CYP51 inhibitor.
Synthesis of polysubstituted (hetero)aromatic compounds enabled by visible-light-promoted radical triple bond insertions has been reviewed. A series of polysubstituted naphthols, furans and isoquinolones were prepared using radical alkyne insertions. 6-Substituted phenanthridine and 1-substituted isoquinoline and pyridine derivatives were synthesized assisted by radical isocyanide insertions. Furthermore, a wide scope of quinoline and quinoxaline derivatives were synthesized assisted by domino radical isocyanide/alkyne insertions and isocyanide/cyano insertions respectively. All reactions could be carried out under visible light photoredox catalysis with good to excellent chemical yields.
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