Synthesis and pharmacological activities of xanthone derivatives as alpha-glucosidase inhibitors.
Considerable interest has been attracted in xanthone and its derivatives because of their large variety of pharmacological activities. In this project, a series of hydroxylxanthones and their acetoxy and alkoxy derivatives were synthesized and evaluated as alpha-glucosidase inhibitors, aimed at clarifying the structure-activity correlation. The results indicated that these xanthone derivatives were capable of inhibiting in vitro alpha-glucosidase with moderate to good activities. Among them, polyhydroxylxanthones exhibited the highest activities and thus may be exploitable as a lead compound for the development of potent alpha-glucosidase inhibitors.
Liu
Yan
Y
School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou, PR China.
Zou
Lan
L
Ma
Lin
L
Chen
Wen-Hua
WH
Wang
Bo
B
Xu
Zun-Le
ZL
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D065089:Glycoside Hydrolase Inhibitors; D012441:Saccharomyces cerevisiae / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D044004:Xanthones / Q000138:chemical synthesis / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D065089:Glycoside Hydrolase Inhibitors; D044004:Xanthones