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Eur J Med Chem. 2015 Jan 27;90:10-20. doi: 10.1016/j.ejmech.2014.11.015. Epub 2014 Nov 6.

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

Author information

1
Department of Chemistry, East China Normal University, 500 Dongchuan Road, Shanghai 200241, China.
2
CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
3
Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai 200241, China.
4
Department of Chemistry, East China Normal University, 500 Dongchuan Road, Shanghai 200241, China. Electronic address: wwqiu@chem.ecnu.edu.cn.

Abstract

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 μg/mL against strain Newman, 45 and 52 showed the most potent activity with MIC values of 0.71-3.12 μg/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.

KEYWORDS:

Antibacterial; Cyclization reaction; Diterpene derivative; Multidrug-resistant; Synthesis

PMID:
25461307
DOI:
10.1016/j.ejmech.2014.11.015
[Indexed for MEDLINE]

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