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

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

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

Bioorg Med Chem. 2012 Aug 1;20(15):4661-7. doi: 10.1016/j.bmc.2012.06.011. Epub 2012 Jun 15.

PubMed ID
22750010 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
BosentanEndothelin-1 receptorIC 50 (nM)8.9N/AN/ADetails