Lack of novel antifungal agents and severe drug resistance has led to high incidence and associated mortality of invasive fungal infections. To tackle the challenges, novel antifungal agents with anti‐resistant potency are highly desirable. Thus, derivatives of curcumin were synthesized to restore the effectiveness of fluconazole (FLC) against FLC‐resistant Candida spp. and structure‐activity relationships were then discussed. Some novel derivatives showed promising features as novel antifungal lead compounds. Of them, compound 4 showed good alone or synergistic antifungal activity against FLC‐resistant Candida spp. Moreover, compound 4 was proven as a potent inhibitor of Candida albicans biofilm formation and yeast‐to‐hypha morphological transition whether used alone or in combination with FLC, which was further confirmed by the inhibitory effect on cellular surface hydrophobicity of C. albicans. Compound 4 also inhibits intracellular ATP production of C. albicans and disrupts membrane permeability of C. albicans when used in combination with FLC. The results highlighted the potential of curcumin derivatives to overcome fluconazole‐related and biofilm‐related drug resistance.
In the presence of the Suginome reagent (PhMe 2 SiÀ Bpin), a large panel of electron-withdrawing alkenes was successfully converted into the hydrosilylated product in good to excellent yields. This direct electrochemical hydrosilylation does not require exogenous oxidants and catalysts. Preliminary mechanistic study supported the involvement of a silyl radical, which reacted on the alkene.
Azoles and organoselenium compounds are pharmacologically
important
scaffolds in medicinal chemistry and natural products. We developed
an efficient regioselective electrochemical aminoselenation reaction
of 1,3-dienes, azoles, and diselenide derivatives to access selenium-containing
allylazoles skeletons. This protocol is more economical and environmentally
friendly and features a broad substrate scope; pyrazole, triazole,
and tetrazolium were all tolerated under the standard conditions,
which could be applied to the expedient synthesis of bioactive molecules
and in the pharmaceutical industry.
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