Literature DB >> 22750010

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

Renren Bai1, Zhen Wei, Jie Liu, Weijia Xie, Hequan Yao, Xiaoming Wu, Jieyun Jiang, Qiujuan Wang, Jinyi Xu.   

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.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22750010     DOI： 10.1016/j.bmc.2012.06.011

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  5 in total

1.  Synthesis, anti-proliferative activity, SAR study, and preliminary in vivo toxicity study of substituted N,N'-bis(arylmethyl)benzimidazolium salts against a panel of non-small cell lung cancer cell lines.

Authors:  Kerri L Shelton; Michael A DeBord; Patrick O Wagers; Marie R Southerland; Travis M Williams; Nikki K Robishaw; Leah P Shriver; Claire A Tessier; Matthew J Panzner; Wiley J Youngs
Journal:  Bioorg Med Chem       Date:  2016-11-05       Impact factor: 3.641

2.  Structural Comparison of Sulfonamide-Based Derivatives That Can Improve Anti-Coagulation Properties of Metformin.

Authors:  Agnieszka Zajda; Joanna Sikora; Kristiina M Huttunen; Magdalena Markowicz-Piasecka
Journal:  Int J Mol Sci       Date:  2022-04-08       Impact factor: 6.208

3.  Endothelium-independent vasodilator effect of isocorynoxeine in vitro isolated from the hook of Uncaria rhynchophylla (Miquel).

Authors:  Ting Li; Ke Xu; Delu Che; Zhuangzhuang Huang; Nabila Jahan; Sicen Wang
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2018-08-02       Impact factor: 3.000

4.  Single-stage synthesis of heterocyclic alkaloid-like compounds from (+)-camphoric acid and their antiviral activity.

Authors:  Vladimir V Chernyshov; Olga I Yarovaya; Dmitry S Fadeev; Yuriy V Gatilov; Yana L Esaulkova; Anna S Muryleva; Katherina O Sinegubova; Vladimir V Zarubaev; Nariman F Salakhutdinov
Journal:  Mol Divers       Date:  2019-02-28       Impact factor: 2.943

5.  4-(2-(1H-Benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamides: design, synthesis and biological evaluation.

Authors:  Sumit Tahlan; Kalavathy Ramasamy; Siong Meng Lim; Syed Adnan Ali Shah; Vasudevan Mani; Balasubramanian Narasimhan
Journal:  BMC Chem       Date:  2019-02-02
  5 in total

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