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Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands
- Authors
- Park, HG; Choi, JY; Kim, MH; Choi, SH; Park, MK; Lee, J; Suh, YG; Cho, HW; Oh, U; Kim, HD; Joo, YH; Shin, SS; Kim, JK; Jeong, YS; Koh, HJ; Park, YH; Jew, SS
- Issue Date
- Feb-2005
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- vanilloid receptor; antagonist; structure-activity relationship
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.15, no.3, pp 631 - 634
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 15
- Number
- 3
- Start Page
- 631
- End Page
- 634
- ISSN
- 0960-894X
1464-3405
- 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 I 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-tet-t-butylphenyl)-4-(3-methylpyridine-2-yl)benzamide (3g, IC50 = 31 nM), showed 5-fold higher antagonistic activity than 1 in Ca-45 (2+)-influx assay. (C) 2004 Elsevier Ltd. All rights reserved.
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