Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands

H Park, J Choi, M Kim, S Choi, M Park, J Lee…

文献索引：Park, Hyeung-Geun; Choi, Ji-Yeon; Kim, Mi-Hyun; Choi, Sea-Hoon; Park, Mi-Kyung; Lee, Jihye; Suh, Young-Ger; Cho, Hawon; Oh, Uhtaek; Kim, Hee-Doo; Joo, Yung Hyup; Shin, Song Seok; Kim, Jin Kwan; Jeong, Yeon Su; Koh, Hyun-Ju; Park, Young-Ho; Jew, Sang-Sup Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 631 - 634

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被引用次数: 16

摘要

Seventeen biarylcarboxybenzamide derivatives were prepared for the study of their agonistic/antagonistic activities to the vanilloid receptor (VR1) in rat DRG neurons. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. Among the prepared derivatives, N-(4-tert-butylphenyl)-4- pyridine-2-yl-benzamide (2, IC50= 31nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2 ...