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. 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

Li-Gang Yu  1 , Teng-Feng Ni  2 , Wei Gao  1 , Yuan He  3 , Ying-Ying Wang  1 , Hai-Wei Cui  1 , Cai-Guang Yang  2 , Wen-Wei Qiu  4
Affiliations

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

Li-Gang Yu et al. Eur J Med Chem. .

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.

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