Efficient synthesis of functionalized dithiocarbamate derivatives through one-pot three-component reaction and evaluation of their antimicrobial activities

摘要

The one-pot three-component reaction of primary and secondary amines, carbon disulfide and β-nitrostyrene derivatives in neat condition at room temperature afforded functionalized dithiocarbamate derivatives in good to high yields. High bond-forming efficiency and easy work-up are advantages of this reaction. In vitro antimicrobial activities of synthesized compounds were studied against four Gram-positive bacteria, four Gram-negative bacteria and four fungi. The screening for the antimicrobial activity was performed by twofold serial dilution technique. Notably, some synthesized compounds displayed comparable or even better antibacterial and antifungal activities against some tested strains than the reference drugs ampicillin, streptomycin and amphotericin B, respectively. Graphical abstract: A series of novel dithiocarbamates 4a-j have been synthesized via three-component reaction and compared pharmacologically concerning their antimicrobial and antibacterial activities as well as antifungal activity [Figure not available: see fulltext.].