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

Li Gang Yu; Teng Feng Ni; Wei Gao; Yuan He; Ying Ying Wang; Hai Wei Cui; Cai Guang Yang; Wen Wei Qiu

doi:10.1016/j.ejmech.2014.11.015

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

Li Gang Yu
, Teng Feng Ni
, Wei Gao
, Yuan He
, Ying Ying Wang
, Hai Wei Cui
, Cai Guang Yang
, Wen Wei Qiu^*

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

Research output: Contribution to journal › Article › peer-review

52 Scopus citations

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.

Original language	English
Pages (from-to)	10-20
Number of pages	11
Journal	European Journal of Medicinal Chemistry
Volume	90
DOIs	https://doi.org/10.1016/j.ejmech.2014.11.015
State	Published - 27 Jan 2015

Keywords

Antibacterial
Cyclization reaction
Diterpene derivative
Multidrug-resistant
Synthesis

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10.1016/j.ejmech.2014.11.015

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title = "The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives",

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",

author = "Yu, \{Li Gang\} and Ni, \{Teng Feng\} and Wei Gao and Yuan He and Wang, \{Ying Ying\} and Cui, \{Hai Wei\} and Yang, \{Cai Guang\} and Qiu, \{Wen Wei\}",

note = "Publisher Copyright: {\textcopyright} 2014 Published by Elsevier Masson SAS.",

year = "2015",

month = jan,

day = "27",

doi = "10.1016/j.ejmech.2014.11.015",

language = "英语",

volume = "90",

pages = "10--20",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

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TY - JOUR

T1 - The synthesis and antibacterial activity of pyrazole-fused tricyclic diterpene derivatives

AU - Yu, Li Gang

AU - Ni, Teng Feng

AU - Gao, Wei

AU - He, Yuan

AU - Wang, Ying Ying

AU - Cui, Hai Wei

AU - Yang, Cai Guang

AU - Qiu, Wen Wei

PY - 2015/1/27

Y1 - 2015/1/27

N2 - 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.

AB - 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.

KW - Antibacterial

KW - Cyclization reaction

KW - Diterpene derivative

KW - Multidrug-resistant

KW - Synthesis

UR - https://www.scopus.com/pages/publications/84909960152

U2 - 10.1016/j.ejmech.2014.11.015

DO - 10.1016/j.ejmech.2014.11.015

M3 - 文章

C2 - 25461307

AN - SCOPUS:84909960152

SN - 0223-5234

VL - 90

SP - 10

EP - 20

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

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

Abstract

Keywords

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