Literature DB >> 20434334

Benzothiophene containing Rho kinase inhibitors: Efficacy in an animal model of glaucoma.

Robert L Davis1, Mehmet Kahraman, Thomas J Prins, Yan Beaver, Travis G Cook, Jessica Cramp, Charmagne S Cayanan, Elisabeth M M Gardiner, Marsha A McLaughlin, Abbot F Clark, Mark R Hellberg, Andrew K Shiau, Stewart A Noble, Allen J Borchardt.   

Abstract

We identified a new benzothiophene containing Rho kinase inhibitor scaffold in an ultra high-throughput enzymatic activity screen. SAR studies, driven by a novel label-free cellular impedance assay, were used to derive 39, which substantially reduced intraocular pressure in a monkey model of glaucoma-associated ocular hypertension. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20434334     DOI: 10.1016/j.bmcl.2010.04.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.

Authors:  Rebecca K Donegan; Raquel L Lieberman
Journal:  J Med Chem       Date:  2015-09-25       Impact factor: 7.446

Review 2.  Discovery of novel inhibitors for the treatment of glaucoma.

Authors:  Kishore Cholkar; Hoang M Trinh; Dhananjay Pal; Ashim K Mitra
Journal:  Expert Opin Drug Discov       Date:  2015-01-09       Impact factor: 6.098

3.  Rho-Rho kinase pathway in the actomyosin contraction and cell-matrix adhesion in immortalized human trabecular meshwork cells.

Authors:  C Ramachandran; R V Patil; K Combrink; N A Sharif; S P Srinivas
Journal:  Mol Vis       Date:  2011-07-14       Impact factor: 2.367

4.  Discovery of Novel ROCK1 Inhibitors via Integrated Virtual Screening Strategy and Bioassays.

Authors:  Mingyun Shen; Sheng Tian; Peichen Pan; Huiyong Sun; Dan Li; Youyong Li; Hefeng Zhou; Chuwen Li; Simon Ming-Yuen Lee; Tingjun Hou
Journal:  Sci Rep       Date:  2015-11-16       Impact factor: 4.379

5.  Synthesis and Evaluation of 3-Halobenzo[b]thiophenes as Potential Antibacterial and Antifungal Agents.

Authors:  Prerna J Masih; Tanay Kesharwani; Elivet Rodriguez; Mia A Vertudez; Mina L Motakhaveri; Terelan K Le; Minh Kieu T Tran; Matthew R Cloyd; Cory T Kornman; Aimee M Phillips
Journal:  Pharmaceuticals (Basel)       Date:  2021-12-28
  5 in total

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