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 virulence factors production in Pseudomonas aeruginosa, essential for pathogenesis. Compound 11b showed the best activity among all the new compounds.
Wang
Zhongli
Z
Institute of New Drug Research and Guangdong Province Key Laboratory of Pharmacodynamic Constituents of Traditional Chinese Medicine and New Drug Research, Jinan University College of Pharmacy, Guangzhou 510632, China.
Yu
Pei
P
Zhang
Gaoxiao
G
Xu
Lipeng
L
Wang
Dingyuan
D
Wang
Liang
L
Zeng
Xiangping
X
Wang
Yuqiang
Y
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002264:Carboxylic Acids / Q000737:chemistry; D004224:Diterpenes / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D011550:Pseudomonas aeruginosa / Q000378:metabolism; D011710:Pyocyanine / Q000037:antagonists & inhibitors / Q000378:metabolism; D053038:Quorum Sensing / Q000187:drug effects; D013329:Structure-Activity Relationship
C552761:14-(5-cyclopentylvaleryl)andrographolide; D000900:Anti-Bacterial Agents; D002264:Carboxylic Acids; D004224:Diterpenes; C030419:andrographolide; D011710:Pyocyanine