编号 020033602
推送时间 20220328
研究领域 林产化工
年份 2022
类型 期刊
语种 英语
标题 Synthetic modifications of abietane diterpene acids to potent antimicrobial agents
来源期刊 Natural Product Research
期 第336期
发表时间 20210827
关键词 Dihydroquinopimaric acid; maleopimaric acid; antimicrobial activity; antitubercular activity; M; tuberculosis H(37)Rv; antifungal activity; docking studies;
摘要 Among abietane type semisynthetic diterpenoids, a series of quinopimaric and maleopimaric acid derivatives modified at the carboxyl and carbonyl groups, and in ring E were synthesised to obtain new compounds with antimicrobial potency against Mycobacterium tuberculosis H(37)Rv and key ESKAPE pathogens. It was found that compound 8 exhibited low toxicity to human embryonic kidney cell line HEK-293 (> 32 mu g/mL) and showed significant bacteriostatic activity against methicillin-resistant Staphylococcus aureus (MRSA) (MIC <= 0.25 mu g/mL) and excellent antifungal activity against Cryptococcus neoformans var. grubii (MICs <= 0.25 mu g/mL) being approximate to 4 and approximate to 30 fold more active than vancomycin and fluconazole. It also showed moderate activity against fungus Candida albicans (MIC <= 0.25 mu g/mL). Compound 9 inhibited M. tuberculosis H(37)Rv with MIC of 1.25 mu g/mL. The docking studies suggest possible interactions of the leading compounds with the molecular targets.
服务人员 尚玮姣
服务院士 宋湛谦
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