Synthesis and Biological Evaluation of Dihydroisoquinoline-2(1H)- Carbothioamide Derivatives as TRPV1 Antagonists

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

Journal Name: Letters in Drug Design & Discovery

Volume 7 , Issue 4 , 2010


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Abstract:

TRPV1 receptor is an important analgesia target. Its antagonists are expected to prevent pain perception by blocking the receptor directly. In this letter, eight dihydroisoquinoline-2(1H)-carbothioamide derivatives were designed and synthesized as TRPV1 antagonists. The benzene ring was modified with different substitutional groups. Preliminary biological tests suggested that the new compounds exhibited TRPV1 antagonist activity and different analgesia effects, some of which were promising as analgesia drugs.

Keywords: TRPV1, Antagonist, Dihydroisoquinoline-2(1H)-carbothioamide, Analgesia

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Article Details

VOLUME: 7
ISSUE: 4
Year: 2010
Page: [235 - 237]
Pages: 3
DOI: 10.2174/157018010790945797
Price: $65

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