Literature DB >> 24900192

Discovery of Potent and Selective Urea-Based ROCK Inhibitors and Their Effects on Intraocular Pressure in Rats.

Yan Yin1, Michael D Cameron1, Li Lin1, Susan Khan1, Thomas Schröter1, Wayne Grant1, Jennifer Pocas1, Yen Ting Chen1, Stephan Schürer2, Alok Pachori1, Philip LoGrasso1, Yangbo Feng1.   

Abstract

A series of urea-based Rho kinase (ROCK) inhibitors were designed and evaluated. The discovered compounds had excellent enzyme and cellular potency, high kinase selectivity, high aqueous solubility, good porcine corneal penetration, and appropriate DMPK profiles for topical applications as antiglaucoma therapeutics.

Entities:  

Keywords:  Glaucoma; IOP; ROCK; kinase inhibitor; pyrazole; urea

Year:  2010        PMID： 24900192      PMCID： PMC4007833          DOI： 10.1021/ml1000382

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  18 in total

Review 1.  Molecular design for enhancement of ocular penetration.

Authors:  Yoshihisa Shirasaki
Journal:  J Pharm Sci       Date:  2008-07       Impact factor: 3.534

2.  Detection of myosin light chain phosphorylation--a cell-based assay for screening Rho-kinase inhibitors.

Authors:  Thomas Schröter; Evelyn Griffin; Amiee Weiser; Yangbo Feng; Philip LoGrasso
Journal:  Biochem Biophys Res Commun       Date:  2008-07-16       Impact factor: 3.575

3.  ROCK-I and ROCK-II, two isoforms of Rho-associated coiled-coil forming protein serine/threonine kinase in mice.

Authors:  O Nakagawa; K Fujisawa; T Ishizaki; Y Saito; K Nakao; S Narumiya
Journal:  FEBS Lett       Date:  1996-08-26       Impact factor: 4.124

4.  Dose response and duration of action of dorzolamide, a topical carbonic anhydrase inhibitor.

Authors:  E A Lippa; L E Carlson; B Ehinger; L O Eriksson; K Finnström; C Holmin; S E Nilsson; K Nyman; C Raitta; A Ringvold
Journal:  Arch Ophthalmol       Date:  1992-04

5.  Reduction of intraocular pressure by topical administration of an inhibitor of the Rho-associated protein kinase.

Authors:  M Waki; Y Yoshida; T Oka; M Azuma
Journal:  Curr Eye Res       Date:  2001-06       Impact factor: 2.424

6.  The number of people with glaucoma worldwide in 2010 and 2020.

Authors:  H A Quigley; A T Broman
Journal:  Br J Ophthalmol       Date:  2006-03       Impact factor: 4.638

7.  The mechanism of timolol in lowering intraocular pressure. In the normal eye.

Authors:  R L Coakes; R F Brubaker
Journal:  Arch Ophthalmol       Date:  1978-11

8.  Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors.

Authors:  Yangbo Feng; Yan Yin; Amiee Weiser; Evelyn Griffin; Michael D Cameron; Li Lin; Claudia Ruiz; Stephan C Schürer; Toshihiro Inoue; P Vasanth Rao; Thomas Schröter; Philip Lograsso
Journal:  J Med Chem       Date:  2008-10-04       Impact factor: 7.446

9.  Comparison of miniaturized time-resolved fluorescence resonance energy transfer and enzyme-coupled luciferase high-throughput screening assays to discover inhibitors of Rho-kinase II (ROCK-II).

Authors:  Thomas Schröter; Dmitriy Minond; Amiee Weiser; Chinh Dao; Jeff Habel; Timothy Spicer; Peter Chase; Pierre Baillargeon; Louis Scampavia; Stephan Schürer; Caty Chung; Chris Mader; Mark Southern; Nick Tsinoremas; Philip LoGrasso; Peter Hodder
Journal:  J Biomol Screen       Date:  2008-01

10.  Effects of brimonidine on aqueous humor dynamics in human eyes.

Authors:  C B Toris; M L Gleason; C B Camras; M E Yablonski
Journal:  Arch Ophthalmol       Date:  1995-12
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  8 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

2.  In silico prediction of ROCK II inhibitors by different classification approaches.

Authors:  Chuipu Cai; Qihui Wu; Yunxia Luo; Huili Ma; Jiangang Shen; Yongbin Zhang; Lei Yang; Yunbo Chen; Zehuai Wen; Qi Wang
Journal:  Mol Divers       Date:  2017-08-02       Impact factor: 2.943

3.  Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.

Authors:  Yan Yin; Ke Zheng; Nibal Eid; Shannon Howard; Ji-Hak Jeong; Fei Yi; Jia Guo; Chul Min Park; Mathieu Bibian; Weilin Wu; Pamela Hernandez; HaJeung Park; Yuntao Wu; Jun-Li Luo; Philip V LoGrasso; Yangbo Feng
Journal:  J Med Chem       Date:  2015-02-04       Impact factor: 7.446

4.  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 5.  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

Review 6.  LIM Kinases, Promising but Reluctant Therapeutic Targets: Chemistry and Preclinical Validation In Vivo.

Authors:  Rayan Berabez; Sylvain Routier; Hélène Bénédetti; Karen Plé; Béatrice Vallée
Journal:  Cells       Date:  2022-06-30       Impact factor: 7.666

7.  Ca2+ sensitization pathways accessed by cholinergic neurotransmission in the murine gastric fundus.

Authors:  Bhupal P Bhetwal; Kenton M Sanders; Changlong An; Danielle M Trappanese; Robert S Moreland; Brian A Perrino
Journal:  J Physiol       Date:  2013-04-22       Impact factor: 5.182

Review 8.  Targeting Schlemm's Canal in the Medical Therapy of Glaucoma: Current and Future Considerations.

Authors:  Vanessa Andrés-Guerrero; Julián García-Feijoo; Anastasios Georgios Konstas
Journal:  Adv Ther       Date:  2017-03-27       Impact factor: 3.845
  8 in total

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