The antimicrobial activity of cyclopropene derivatives towards oral bacteria

Abstract

The aim of this study was to synthesize cyclopropene derivatives and evaluate their oral antimicrobial activities. Nine cyclopropene derivatives possessing various functional groups as substituents on a ring were prepared by rhodium-catalyzed cycloaddition reaction in moderate yields. Among them, six typical cyclopropenes were shown to have antimicrobial activities against Gram-positive and Gram-negative bacteria including Staphylococcus aureus, Bacillus cereus and Escherichia coli. We evaluated in turn their inhibitory effects against oral bacteria and all nine compounds were elucidated to have potent inhibitory effects on the growth of oral bacterial flora derived from human whole saliva under aerobic and anaerobic conditions. In addition, four typical cyclopropenes of these compounds were shown to exhibit strong antimicrobial activities against Porphyromonas gingivalis and Streptococcus sobrinus. These results indicate that cyclopropene derivatives were promising agents for the prevention and treatment of dental caries and periodontal diseases.