摘要
To study structure-activity relationship of rhodomyrtone against Gram-positive bacteria, structural modification of rhodo- myrtone was carded out to afford its 10 analogues. All compounds were assayed for their antibacterial potency using broth microdilution method. The results indicated that rhodomyrtone exhibited higher antibacterial activity against al! Gram-positive bacteria than its analogues, with the exception of rhodomyrtone 6,8-diacetate (3) and oxime analogues 6 and 7 which demonstrated similar activity as the parent compound against Bacillus subtilis and Staphylococcus epidermidis with minimum inhibitory concentration and minimum bactericidal concentration ranged from 1 to 4 ~g/mL and 2 to 4 ~g/mL, respectively. In contrast, all analogues displayed no activity against Acinetobacter baumannii. Hydroxyl and ketone groups of rhodomyrtone were elucidated to be essential for the antibacterial property.
To study structure-activity relationship of rhodomyrtone against Gram-positive bacteria, structural modification of rhodo- myrtone was carded out to afford its 10 analogues. All compounds were assayed for their antibacterial potency using broth microdilution method. The results indicated that rhodomyrtone exhibited higher antibacterial activity against al! Gram-positive bacteria than its analogues, with the exception of rhodomyrtone 6,8-diacetate (3) and oxime analogues 6 and 7 which demonstrated similar activity as the parent compound against Bacillus subtilis and Staphylococcus epidermidis with minimum inhibitory concentration and minimum bactericidal concentration ranged from 1 to 4 ~g/mL and 2 to 4 ~g/mL, respectively. In contrast, all analogues displayed no activity against Acinetobacter baumannii. Hydroxyl and ketone groups of rhodomyrtone were elucidated to be essential for the antibacterial property.
基金
the Royal Golden Jubilee Ph.D. Program(No.PHD/0023/255 1),Prince of Songkla University
the National Research University Project of Thailand's Office ofthe Higher Education Commission for financial support
Support from the Center of Excellence for Innovation in Chemistry is gratefully acknowledged