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Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.

Abstract：

:A series of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives (Ia-Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT(1) and endothelin ET(A) receptors (AT(1) IC(50)=8.5, ET(A) IC(50)=8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure-activity relationships were also discussed in the present paper.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Bai R,Wei Z,Liu J,Xie W,Yao H,Wu X,Jiang J,Wang Q,Xu J

doi

10.1016/j.bmc.2012.06.011

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

4661-7

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00489-0

journal_volume

20

pub_type

杂志文章

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