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

…, H Zhang, J Zhou, W Huang, J Jin, D Dai

文献索引：Qian, Hai; Chen, Wei; Zhang, Xiaoyan; Zhang, Huibin; Zhou, Jinpei; Huang, Wenlong; Jin; Dai, Dongyan Letters in Drug Design and Discovery, 2010 , vol. 7, # 4 p. 235 - 237

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摘要

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 ...