4'-[(苯并咪唑-1-基)甲基]联苯-2-磺酰胺衍生物的合成及作为双重血管紧张素 II/内皮素 A 受体拮抗剂的生物评价。
Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
机构信息
Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
出版信息
Bioorg Med Chem. 2012 Aug 1;20(15):4661-7. doi: 10.1016/j.bmc.2012.06.011. Epub 2012 Jun 15.
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.
一系列 4'-[(苯并咪唑-1-基)甲基]联苯-2-磺酰胺衍生物（Ia-Il）被合成并进行了生物学评价。结果发现，活性最强的化合物 Ig 对血管紧张素 II AT(1)和内皮素 ET(A)受体均具有拮抗作用（AT(1)IC(50)=8.5，ET(A)IC(50)=8.9 nM），且在 RHR 中比氯沙坦更有效，对心率无明显影响。本文还讨论了初步的构效关系。
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