Synthetic modifications of abietane diterpene acids to potent antimicrobial agents

编号 020030901

推送时间 20210920

研究领域 林产化工 

年份 2021 

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309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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