Discovery of Novel 2 ',3 ',4 '-Trihydroxy-2-phenylacetophenone Derivatives as Anti-Gram-Positive Antibacterial Agents

作者：Goto Hideyuki; Kumada Yuji; Ashida Hitoshi; Yoshida Ken ichi^*

来源：Bioscience Biotechnology and Biochemistry, 2009, 73(1): 124-128.

DOI：10.1271/bbb.80532

• antibacterial agent
• 2-phenylacetophenone
• Gram-positive
• Staphylococcus aureus

A number of 2',3',4'-trihydroxy-2-phenylacetophenone derivatives were synthesized and examined for growth inhibition of several kinds of bacteria. 2',3',4'-Trihydroxy-2-phenylacetophenone itself exhibited no antibacterial activity, but some of its derivatives showed various antibacterial activities depending on functional groups introduced on the 2-phenyl ring. Eighteen out of 24 compounds synthesized in this study appeared to possess antibacterial activities against at least two Gram-positive strains of Bacillus subtilis and Staphylococcus aureus, 2-(biphenyl-4-yl)-2',3',4'-trihydroxy-acetophenone being the most active with LC50 of 5.8 mu M and 5.6 mu M respectively. However, none of the synthesized compounds exhibited inhibitory effects on Gram-negative strains, such as Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, and Salmonella enterica, suggesting that anti-Gram-positive specificity of the antibacterial compounds.

• 出版日期2009-1