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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Jing Li

Volume 8, Issue 9, 2011

Page: [816 - 821] Pages: 6

DOI: 10.2174/157018011797200740

Price: $65

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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