Design and synthesis of aralkyl-ketone piperazine derivatives and their antalgic activities.
- Author:
Jian-qi LI
1
;
Li-ying HUANG
;
Jian-xin CHEN
;
Zhi-jie WENG
;
Chun-nian ZHANG
Author Information
1. Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China. lijq@sipi.com.cn
- Publication Type:Journal Article
- MeSH:
Analgesics;
chemical synthesis;
pharmacology;
Animals;
Female;
Male;
Mice;
Molecular Structure;
Pain Measurement;
Piperazines;
chemical synthesis;
pharmacology;
Random Allocation;
Rats;
Rats, Sprague-Dawley
- From:
Acta Pharmaceutica Sinica
2007;42(11):1166-1175
- CountryChina
- Language:Chinese
-
Abstract:
To synthesize aralkyl-ketone piperazine derivatives as analgesic agents, the N atom of the one side of piperazine ring is protected by formyl group firstly, then the unprotected N atom is alkylated to prepare aralkyl-ketone piperazine derivatives. Their analgesic biological activities were well studied by mice writhing model, rat hot plate model and rat tail flick model. Sixty four compounds were synthesized and pharmacological tests in vivo revealed these compounds have potent analgesic activities, especially compound I12, I14, I14 I21 and I37. These four compounds are more worthy for further research.
