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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Synthesis and Biological Evaluation of Capsaicin Derivatives as Analgesia Drugs

Author(s): Hai Qian, Zhixian Fu, Huibin Zhang, Jinpei Zhou, Wenlong Huang, Jing Jin, Wei Chen and Dongyan Dai

Volume 7, Issue 2, 2010

Page: [122 - 127] Pages: 6

DOI: 10.2174/157018010790225822

Price: $65


TRPV1 is an important analgesia target. Capsaicin, the prototypical TRPV1 agonist, has a clear therapeutic potential. But the highly pungency limited its use. In this letter, for lowering its pungency, a series of capsaicin derivatives were designed and synthesized, including 10 compounds which were the direct combination of capsaicin and dihydro capsaicin with various NSAIDs. 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.

Keywords: Analgesia Drugs, Capsaicin Derivatives, TRPV1 Agonist

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