[Design and synthesis of aralkyl-ketone piperazine derivatives and their antalgic activities].
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.
Li
Jian-qi
JQ
Shanghai Institute of Pharmaceutical Industry, Shanghai 200040, China. lijq@sipi.com.cn
Huang
Li-ying
LY
Chen
Jian-xin
JX
Weng
Zhi-jie
ZJ
Zhang
Chun-nian
CN
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D005260:Female; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010147:Pain Measurement; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley
D000700:Analgesics; D010879:Piperazines