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Literature DB >> 20022494

2,3-Diaminopyrazines as Rho kinase inhibitors.

Alan J Henderson¹, Mark Hadden, Cheng Guo, Neema Douglas, Helene Decornez, Mark R Hellberg, Andrew Rusinko, Marsha McLaughlin, Naj Sharif, Colene Drace, Raj Patil.

Abstract

Inhibition of rho kinase (ROCK) has been recognized as an important target for a number of diseases, including glaucoma. Herein we report SAR development around two hits from a kinase library that led to the discovery of the ROCK inhibitor compound 38. In vitro and in vivo analysis of this compound, including its effects in a monkey model of glaucoma will be discussed. Copyright (c) 2009 Elsevier Ltd. All rights reserved.

Entities: Chemical Disease Gene

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Year: 2009 PMID： 20022494 DOI： 10.1016/j.bmcl.2009.12.012

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

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Cited

9 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. Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.

Authors: Najam A Sharif
Journal: ACS Pharmacol Transl Sci Date: 2020-11-05

3. 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 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. A General Method for Nucleophilic Aromatic Substitution of Aryl Fluorides and Chlorides with Dimethylamine using Hydroxide-Assisted Decomposition of N,N-Dimethylforamide.

Authors: Juana Garcia; Jacob Sorrentino; Emily J Diller; Daniel Chapman; Zachary R Woydziak
Journal: Synth Commun Date: 2016-02-09 Impact factor: 2.007

2,3-Diaminopyrazines as Rho kinase inhibitors.

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

2. Discovery to Launch of Anti-allergy (Emadine; Patanol/Pataday/Pazeo) and Anti-glaucoma (Travatan; Simbrinza) Ocular Drugs, and Generation of Novel Pharmacological Tools Such as AL-8810.

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

Review 4. Discovery of novel inhibitors for the treatment of glaucoma.

5. A General Method for Nucleophilic Aromatic Substitution of Aryl Fluorides and Chlorides with Dimethylamine using Hydroxide-Assisted Decomposition of N,N-Dimethylforamide.

6. Amination of heteroaryl chlorides: palladium catalysis or SN Ar in green solvents?

Review 7. Targeting Schlemm's Canal in the Medical Therapy of Glaucoma: Current and Future Considerations.

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

9. Induction of oligodendrocyte differentiation and in vitro myelination by inhibition of rho-associated kinase.