Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VRI) antagonistic figands

被引：19

作者：

Park, HG ^{[1
]}

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

机构：

[1] Seoul Natl Univ, Res Inst Pharmaceut Sci, Seoul 151742, South Korea

[2] Seoul Natl Univ, Coll Pharm, Seoul 151742, South Korea

[3] Sookmyung Womens Univ, Coll Pharm, Seoul 140742, South Korea

[4] AmorePacific R & D Ctr, Youngin Si 449900, Kyounggi, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 03期

关键词：

vanilloid receptor; antagonist; structure-activity relationship;

D O I：

10.1016/j.bmcl.2004.11.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 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.

引用

页码：631 / 634

页数：4

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