Synthesis and structure-activity relationship of rhodomyrtone derivatives as antibacterial agent

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 rhodom...

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Bibliographic Details
Published in:Chinese chemical letters 2012-09, Vol.23 (9), p.1011-1014
Main Authors: Leejae, Sukanlaya, Yingyongnarongkul, Boon-ek, Suksamrarn, Apichart, Voravuthikunchai, Supayang Piyawan
Format: Article
Language:English
Subjects:
Antibacterial activity
Bacillus
Oxime analogues
Rhodomyrtone
Structure–activity relationship
合成
工具
抗菌剂
活性关系
结构
衍生
革兰氏阳性菌
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Summary: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.
ISSN:1001-8417
1878-5964
DOI:10.1016/j.cclet.2012.06.040