Author/Authors :
Hyeung-geun Park، نويسنده , , Ji-yeon Choi، نويسنده , , Mi-Hyun Kim، نويسنده , , Sea-hoon Choi، نويسنده , , Mi-kyung Park، نويسنده , , Jihye Lee، نويسنده , , Young-Ger Suh، نويسنده , , Hawon Cho، نويسنده , , Uhtaek Oh، نويسنده , , Hee-Doo Kim، نويسنده , , Yung Hyup Joo، نويسنده , , Song Seok Shin، نويسنده , , Jin-Kwan Kim، نويسنده , , Yeon Su Jeong، نويسنده , , Hyun-Ju Koh، نويسنده , , Young-Ho Park، نويسنده , , Sang-sup Jew، نويسنده ,
Abstract :
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 = 31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl)benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in 45Ca2+-influx assay.
