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

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

Volume: 7 Issue: 4

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

Affiliation:

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

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.

Cite this article as:

Qian Hai, Chen Wei, Zhang Xiaoyan, Zhang Huibin, Zhou Jinpei, Huang Wenlong, Jin Jing and Dai Dongyan, Synthesis and Biological Evaluation of Dihydroisoquinoline-2(1H)- Carbothioamide Derivatives as TRPV1 Antagonists, Letters in Drug Design & Discovery 2010; 7 (4) . https://dx.doi.org/10.2174/157018010790945797