Literature DB >> 21349713

Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.

Xingang Fang1, Yen Ting Chen, E Hampton Sessions, Sarwat Chowdhury, Tomas Vojkovsky, Yan Yin, Jennifer R Pocas, Wayne Grant, Thomas Schröter, Li Lin, Claudia Ruiz, Michael D Cameron, Philip LoGrasso, Thomas D Bannister, Yangbo Feng.   

Abstract

Rho kinase (ROCK) is an attractive therapeutic target for various diseases including glaucoma, hypertension, and spinal cord injury. Herein, we report the development of a series of ROCK-II inhibitors based on 4-quinazolinone and quinazoline scaffolds. SAR studies at three positions of the quinazoline core led to the identification of analogs with high potency against ROCK-II and good selectivity over protein kinase A (PKA).
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21349713     DOI: 10.1016/j.bmcl.2011.01.039

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


  6 in total

1.  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 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.  Enantioselective synthesis of 3-arylquinazolin-4(3H)-ones via peptide-catalyzed atroposelective bromination.

Authors:  Matthew E Diener; Anthony J Metrano; Shuhei Kusano; Scott J Miller
Journal:  J Am Chem Soc       Date:  2015-09-18       Impact factor: 15.419

4.  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

5.  Synthesis, antitumor activity, 3D-QSAR and molecular docking studies of new iodinated 4-(3H)-quinazolinones 3N-substituted.

Authors:  Marcia Pérez-Fehrmann; Víctor Kesternich; Arturo Puelles; Víctor Quezada; Fernanda Salazar; Philippe Christen; Jonathan Castillo; Juan Guillermo Cárcamo; Alejandro Castro-Alvarez; Ronald Nelson
Journal:  RSC Adv       Date:  2022-08-02       Impact factor: 4.036

Review 6.  New therapeutic targets for intraocular pressure lowering.

Authors:  A Rocha-Sousa; J Rodrigues-Araújo; Petra Gouveia; João Barbosa-Breda; S Azevedo-Pinto; P Pereira-Silva; A Leite-Moreira
Journal:  ISRN Ophthalmol       Date:  2013-07-16
  6 in total

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