Synthesis and biological evaluation of novel pentacyclic triterpene derivatives as potential PPARγ agonists.
Synthesis and biological evaluation of a novel series of substituted pentacyclic triterpene derivatives as potential PPARγ  agoinsts and glycogen phosphorylase inhibitors have been described. Compounds 11 and 17 showed potent PPARγ  agonistic activity and activated the transcription activity of PPARγ  in a dose-dependent manner. On the other hand, eleven compounds exhibited moderate inhibitory activity against rabbit muscle glycogen phosphorylase a (RMGPa), and triterpene 10 was the best one. Structure-activity relationship (SAR) is also discussed.
Institute of Traditional Chinese Medicine, Chengde Medical College, Chengde 067000, People’s Republic of China.
Liying
L
Zhang
Jizhe
J
Dong
Jun
J
Liu
Luyong
L
Zhang
Lingyi
L
Kong
Hequan
H
Yao
Hongbin
H
Sun
D000818:Animals; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000494:pharmacology; D024982:Glycogen Phosphorylase, Muscle Form / Q000037:antagonists & inhibitors*; D006801:Humans; D015394:Molecular Structure; D047495:PPAR gamma / Q000819:agonists*; D053978:Pentacyclic Triterpenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011485:Protein Binding / Q000187:drug effects; D011817:Rabbits; D000077154:Rosiglitazone; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000737:chemistry / Q000494:pharmacology
D004791:Enzyme Inhibitors; D047495:PPAR gamma; D053978:Pentacyclic Triterpenes; D045162:Thiazolidinediones; D000077154:Rosiglitazone; D024982:Glycogen Phosphorylase, Muscle Form