The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives

被引：48

作者：

Yu, Li-Gang ^{[1
]}

Ni, Teng-Feng ^{[2
]}

Gao, Wei ^{[1
]}

He, Yuan ^{[3
,4
]}

Wang, Ying-Ying ^{[1
]}

Cui, Hai-Wei ^{[1
]}

Yang, Cai-Guang ^{[2
]}

Qiu, Wen-Wei ^{[1
]}

机构：

[1] E China Normal Univ, Dept Chem, Shanghai 200241, Peoples R China

[2] Chinese Acad Sci, Shanghai Inst Mat Med, CAS, Key Lab Receptor Res, Shanghai 201203, Peoples R China

[3] E China Normal Univ, Inst Biomed Sci, Shanghai Key Lab Regulatory Biol, Shanghai 200241, Peoples R China

[4] E China Normal Univ, Sch Life Sci, Shanghai 200241, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2015年 / 90卷

关键词：

Antibacterial; Multidrug-resistant; Diterpene derivative; Cyclization reaction; Synthesis; RESISTANT STAPHYLOCOCCUS-AUREUS; ANTIMICROBIAL ACTIVITY; ANACARDIC ACID; TOTAROL; METHICILLIN; CYCLIZATION; BACTERIA;

D O I：

10.1016/j.ejmech.2014.11.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The diterpenoid compound 5 was identified as an antibacterial lead in our screening of small synthetic natural product-like (NPL) library. A series of novel diterpene derivatives were synthesized and investigated for their activity against Staphylococcus aureus Newman strain and multidrug-resistant strains (NRS-1, NRS-70, NRS-100, NRS-108 and NRS-271). Among the compounds tested, 42 and 43 showed highest activity with a MIC of 1 mu g/mL against strain Newman, 45 and 52 showed the most potent activity with MIC values of 0.71-3.12 mu g/mL against five multidrug-resistant S. aureus. All high-antimicrobial active compounds showed no obvious toxicity to human fibroblast (HAF) cells at the MIC concentration. (C) 2014 Published by Elsevier Masson SAS.

引用

页码：10 / 20

页数：11

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