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Letters in Drug Design & Discovery

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

DOI: 10.2174/157018010790945797

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

Page: [235 - 237] Pages: 3

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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