Synthesis and preliminary biological evaluation of capsaicin derivatives as potential analgesic drugs.
A series of capsaicin derivatives were designed and synthesized, including 10 compounds which are the combination of capsaicin and dihydro capsaicin with ibuprofen through bridge chain. Preliminary biological tests suggested that some compounds had both anti-inflammatory activity and analgesic activity. And their pungency was lower. Based on these results, some of these molecules can be considered as lead candidates for the further development of analgesic drugs.
Qian
Hai
H
School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
Fu
Zhixian
Z
Huang
Wenlong
W
Zhang
Huibin
H
Zhou
Jinpei
J
Ge
Liang
L
Lin
Rui
R
Lin
Haiyan
H
Hu
Xiaowen
X
D019342:Acetic Acid / Q000008:administration & dosage; D000284:Administration, Oral; D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002211:Capsaicin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004195:Disease Models, Animal; D015195:Drug Design; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D005260:Female; D006801:Humans; D008297:Male; D051379:Mice; D015394:Molecular Structure; D010146:Pain / Q000139:chemically induced / Q000188:drug therapy*; D051381:Rats; D013237:Stereoisomerism; D050916:TRPV Cation Channels / Q000819:agonists; D014992:Xylenes / Q000008:administration & dosage
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D050916:TRPV Cation Channels; C494482:TRPV1 protein, human; D014992:Xylenes; D019342:Acetic Acid; D002211:Capsaicin