Synthesis and Biological Evaluation of Andrographolide Derivatives as Potent Antibacterial Agents

Title: Synthesis and Biological Evaluation of Andrographolide Derivatives as Potent Antibacterial Agents

Volume: 8 Issue: 9

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

Affiliation:

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

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.

Cite this article as:

Tang Chunlei, Zhang Wenjie, Wang Xinyang, Wang Bin, Zhu Xiaoyun, Huang Dandan, Du Xiaoyong, Qian Hai, Huang Wenlong and Li Jing, Synthesis and Biological Evaluation of Andrographolide Derivatives as Potent Antibacterial Agents, Letters in Drug Design & Discovery 2011; 8 (9) . https://dx.doi.org/10.2174/157018011797200740