Design, synthesis and antibacterial activity of novel andrographolide derivatives

A series of andrographolide derivatives were synthesized through a facile condensation reaction with different carboxylic acids. The new compounds were characterized and screened for their antibacterial activities. A number of the new compounds significantly reduced bacterial quorum sensing virulenc...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2010-06, Vol.18 (12), p.4269-4274
Main Authors: Wang, Zhongli, Yu, Pei, Zhang, Gaoxiao, Xu, Lipeng, Wang, Dingyuan, Wang, Liang, Zeng, Xiangping, Wang, Yuqiang
Format: Article
Language:English
Subjects:
Andrographolide derivatives
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Carboxylic Acids - chemistry
Diterpenes - chemical synthesis
Diterpenes - chemistry
Diterpenes - pharmacology
Drug Design
Medical sciences
Pharmacology. Drug treatments
Pseudomonas aeruginosa - metabolism
Pyocyanine - antagonists & inhibitors
Pyocyanine - metabolism
Quorum sensing
Quorum Sensing - drug effects
Structure-Activity Relationship
Synthesis
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Summary:A series of andrographolide derivatives were synthesized through a facile condensation reaction with different carboxylic acids. The new compounds were characterized and screened for their antibacterial activities. A number of the new compounds significantly reduced bacterial quorum sensing virulence factors production in Pseudomonas aeruginosa, essential for pathogenesis. Compound 11b showed the best activity among all the new compounds.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2010.04.094