Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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Synthesis and Biological Evaluation of Andrographolide Derivatives as Potent Antibacterial Agents

Author(s): Chunlei Tang, Wenjie Zhang, Xinyang Wang, Bin Wang, Xiaoyun Zhu, Dandan Huang, Xiaoyong Du, Hai Qian, Wenlong Huang, Jing Li.

Abstract:

A series of andrographolide (Andro) derivatives (3-14) were designed, synthesized and screened for their antibacterial activities against both gram-positive and gram-negative bacteria in vitro. The most promising compounds 14a-c exhibited at least eight-fold stronger antibacterial activities compared to Andro. Especially, Compound 14a, which showed 32-fold stronger antibacterial activity than Andro, has a potency to be a new lead.

Keywords: Andrographolide, Antibacterial activity, Derivatives, Lactone, P. aeruginosa, Synthesis, bicyclic diterpenoid lactone, Andrographis paniculata, gram-negative bacteria, Elemental analysis, Shimadzu FTIR-8400S spectrometer, TMS standard, MSD spectrometer, LC spectrometer, halohydrocarbon, epigenetics

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Article Details

VOLUME: 8
ISSUE: 9
Year: 2011
Page: [816 - 821]
Pages: 6
DOI: 10.2174/157018011797200740
Price: $58