Literature DB >> 18996009

Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.

E Hampton Sessions1, Yan Yin, Thomas D Bannister, Amiee Weiser, Evelyn Griffin, Jennifer Pocas, Michael D Cameron, Claudia Ruiz, Li Lin, Stephan C Schürer, Thomas Schröter, Philip LoGrasso, Yangbo Feng.   

Abstract

Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.

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Year:  2008        PMID: 18996009     DOI: 10.1016/j.bmcl.2008.10.095

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


  10 in total

Review 1.  Rho-kinase inhibitors as therapeutics: from pan inhibition to isoform selectivity.

Authors:  C Hahmann; T Schroeter
Journal:  Cell Mol Life Sci       Date:  2009-11-12       Impact factor: 9.261

2.  Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).

Authors:  Roberta Pireddu; Kara D Forinash; Nan N Sun; Mathew P Martin; Shen-Shu Sung; Brian Alexander; Jin-Yi Zhu; Wayne C Guida; Ernst Schönbrunn; Saïd M Sebti; Nicholas J Lawrence
Journal:  Medchemcomm       Date:  2012-01-27       Impact factor: 3.597

Review 3.  Potential benefits of rho-kinase inhibition in arterial hypertension.

Authors:  Olaf Grisk
Journal:  Curr Hypertens Rep       Date:  2013-10       Impact factor: 5.369

Review 4.  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

5.  Design, synthesis and in silico screening of benzoxazole-thiazolidinone hybrids as potential inhibitors of SARS-CoV-2 proteases.

Authors:  Vijay Sai Krishna Cheerala; Prasanth Ghanta; Sundaresan Chittor Neelakantan
Journal:  RSC Adv       Date:  2021-12-10       Impact factor: 4.036

6.  Discovery of Novel N-Substituted Prolinamido Indazoles as Potent Rho Kinase Inhibitors and Vasorelaxation Agents.

Authors:  Yangyang Yao; Renze Li; Xiaoyu Liu; Feilong Yang; Ying Yang; Xiaoyu Li; Xiang Shi; Tianyi Yuan; Lianhua Fang; Guanhua Du; Xiaozhen Jiao; Ping Xie
Journal:  Molecules       Date:  2017-10-19       Impact factor: 4.411

Review 7.  Multitargeting the Action of 5-HT6 Serotonin Receptor Ligands by Additional Modulation of Kinases in the Search for a New Therapy for Alzheimer's Disease: Can It Work from a Molecular Point of View?

Authors:  Kinga Czarnota-Łydka; Katarzyna Kucwaj-Brysz; Patryk Pyka; Wawrzyniec Haberek; Sabina Podlewska; Jadwiga Handzlik
Journal:  Int J Mol Sci       Date:  2022-08-07       Impact factor: 6.208

8.  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

9.  Data on the effects of imidazo[1,2-a]benzimidazole and pyrimido[1,2-a]benzimidazole compounds on intraocular pressure of ocular normotensive rats.

Authors:  Adrian Julian Marcus; Igor Iezhitsa; Renu Agarwal; Pavel Vassiliev; Alexander Spasov; Olga Zhukovskaya; Vera Anisimova; Nafeeza Mohd Ismail
Journal:  Data Brief       Date:  2018-03-08

10.  Benzoxazole derivatives: design, synthesis and biological evaluation.

Authors:  Saloni Kakkar; Sumit Tahlan; Siong Meng Lim; Kalavathy Ramasamy; Vasudevan Mani; Syed Adnan Ali Shah; Balasubramanian Narasimhan
Journal:  Chem Cent J       Date:  2018-08-12       Impact factor: 4.215

  10 in total

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