Studies on the novel alpha-glucosidase inhibitory activity and structure-activity relationships for andrographolide analogues.
A series of analogues of andrographolide were synthesized and evaluated as novel alpha-glucosidase inhibitors. Among them compound 23, 15-p-methoxylbenzylidene 14-deoxy-11,12-didehydroandrographolide, was a potent inhibitor against alpha-glucosidase whose IC(50) value was 16microM. The structure-activity relationships were also discussed.
Dai
Gui-Fu
GF
New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450052, PR China.
Xu
Hai-Wei
HW
Wang
Jun-Feng
JF
Liu
Feng-Wu
FW
Liu
Hong-Min
HM
D000818:Animals; D004224:Diterpenes / Q000737:chemistry* / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D051381:Rats; D013329:Structure-Activity Relationship
D004224:Diterpenes; D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; C030419:andrographolide