Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives.
- Author:
Peng XIE
;
Guan WANG
;
Guisen ZHANG
;
Li ZHANG
;
Xiangqing XU
;
Lin GUO
;
Jianqi LI
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2012;47(11):1511-6
- CountryChina
- Language:Chinese
-
Abstract:
To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.
