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Park HG, Choi JY, Kim MH, Choi SH, Park MK, Lee J, Suh YG, Cho H, Oh U, Kim HD, Joo YH, Shin SS, Kim JK, Jeong YS, Koh HJ, Park YH, Jew SS: Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands. Bioorg Med Chem Lett. 2005 Feb 1;15(3):631-4.
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, IC (50)=31 nM) and N-(4-tert-butylphenyl)-4-(3-methylpyridine-2-yl) benzamide (3g, IC (50)=31 nM), showed 5-fold higher antagonistic activity than 1 in (45) Ca (2+)-influx assay. |
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