Synthesis of novel acacetin derivatives and evaluation of their activities
10.13220/j.cnki.jipr.2017.06.021
- VernacularTitle:新的刺槐素衍生物的合成与活性评价
- Author:
Yanjie LI
;
Jing LI
;
Shiyong FAN
;
Menghua LI
;
Yuanyuan ZHOU
;
Bohua ZHONG
;
Weiguo SHI
- Keywords:
acacetin derivative;
synthesis;
analgesic;
writhing
- From:
Journal of International Pharmaceutical Research
2017;44(6):580-584
- CountryChina
- Language:Chinese
-
Abstract:
Objective To improve the in vivo analgesic activity of acacetin and find leads for the development of new drugs, novel acacetin derivatives containing alkyl amide groups with different length of carbon chain were designed and synthesized according to the molecular structure of the active hit compound found in our previous work. Methods Using apigenin as the initial chemical ma-terial,the acacetin was synthesized through 3 steps,then the target compounds were prepared by conjugating hydroxy group of acace-tin at position 7 with bromoalkyl amides. The analgesic activity of the target compounds was evaluated by acetic acid writhing model of mice. Results and Conclusion Novel acacetin alkyl amide derivatives showed more potent analgesic activities than that of clinical medicine diclofenac,which could be used as leads for further development of new drugs.
