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Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.

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Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors. / Schirok, Hartmut; Kast, Raimund; Figueroa-Pérez, Santiago; Bennabi, Samir; Gnoth, Mark J; Feurer, Achim; Heckroth, Heike; Thutewohl, Michael; Paulsen, Holger; Knorr, Andreas; Hütter, Joachim; Lobell, Mario; Münter, Klaus; Geiss, Volker; Ehmke, Heimo; Lang, Dieter; Radtke, Martin; Mittendorf, Joachim; Stasch, Johannes-Peter.

in: CHEMMEDCHEM, Jahrgang 3, Nr. 12, 12, 2008, S. 1893-1904.

Publikationen: SCORING: Beitrag in Fachzeitschrift/Zeitung › SCORING: Zeitschriftenaufsatz › Forschung › Begutachtung

Harvard

Schirok, H, Kast, R, Figueroa-Pérez, S, Bennabi, S, Gnoth, MJ, Feurer, A, Heckroth, H, Thutewohl, M, Paulsen, H, Knorr, A, Hütter, J, Lobell, M, Münter, K, Geiss, V, Ehmke, H, Lang, D, Radtke, M, Mittendorf, J & Stasch, J-P 2008, 'Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.', CHEMMEDCHEM, Jg. 3, Nr. 12, 12, S. 1893-1904. <http://www.ncbi.nlm.nih.gov/pubmed/18973168?dopt=Citation>

APA

Schirok, H., Kast, R., Figueroa-Pérez, S., Bennabi, S., Gnoth, M. J., Feurer, A., Heckroth, H., Thutewohl, M., Paulsen, H., Knorr, A., Hütter, J., Lobell, M., Münter, K., Geiss, V., Ehmke, H., Lang, D., Radtke, M., Mittendorf, J., & Stasch, J-P. (2008). Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors. CHEMMEDCHEM, 3(12), 1893-1904. [12]. http://www.ncbi.nlm.nih.gov/pubmed/18973168?dopt=Citation

Vancouver

Schirok H, Kast R, Figueroa-Pérez S, Bennabi S, Gnoth MJ, Feurer A et al. Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors. CHEMMEDCHEM. 2008;3(12):1893-1904. 12.

Bibtex

@article{d385e18db4d8470589480fe3b15f57e0,
title = "Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.",
abstract = "Rho kinase plays a pivotal role in several cellular processes such as vasoregulation, making it a suitable target for the treatment of hypertension and related disorders. We discovered a new compound class of Rho kinase (ROCK) inhibitors containing a 7-azaindole hinge-binding scaffold tethered to an aminopyrimidine core. Herein we describe the structure-activity relationships elucidated through biochemical and functional assays. The introduction of suitable substituents at the 3-position of the bicyclic moiety led to an increase in activity, which was required to design compounds with favorable pharmacokinetic profile. Azaindole 32 was identified as a highly selective and orally available ROCK inhibitor able to cause a sustained blood pressure reduction in vivo.",
author = "Hartmut Schirok and Raimund Kast and Santiago Figueroa-P{\'e}rez and Samir Bennabi and Gnoth, {Mark J} and Achim Feurer and Heike Heckroth and Michael Thutewohl and Holger Paulsen and Andreas Knorr and Joachim H{\"u}tter and Mario Lobell and Klaus M{\"u}nter and Volker Geiss and Heimo Ehmke and Dieter Lang and Martin Radtke and Joachim Mittendorf and Johannes-Peter Stasch",
year = "2008",
language = "Deutsch",
volume = "3",
pages = "1893--1904",
journal = "CHEMMEDCHEM",
issn = "1860-7179",
publisher = "John Wiley and Sons Ltd",
number = "12",

}

RIS

TY - JOUR

T1 - Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.

AU - Schirok, Hartmut

AU - Kast, Raimund

AU - Figueroa-Pérez, Santiago

AU - Bennabi, Samir

AU - Gnoth, Mark J

AU - Feurer, Achim

AU - Heckroth, Heike

AU - Thutewohl, Michael

AU - Paulsen, Holger

AU - Knorr, Andreas

AU - Hütter, Joachim

AU - Lobell, Mario

AU - Münter, Klaus

AU - Geiss, Volker

AU - Ehmke, Heimo

AU - Lang, Dieter

AU - Radtke, Martin

AU - Mittendorf, Joachim

AU - Stasch, Johannes-Peter

PY - 2008

Y1 - 2008

N2 - Rho kinase plays a pivotal role in several cellular processes such as vasoregulation, making it a suitable target for the treatment of hypertension and related disorders. We discovered a new compound class of Rho kinase (ROCK) inhibitors containing a 7-azaindole hinge-binding scaffold tethered to an aminopyrimidine core. Herein we describe the structure-activity relationships elucidated through biochemical and functional assays. The introduction of suitable substituents at the 3-position of the bicyclic moiety led to an increase in activity, which was required to design compounds with favorable pharmacokinetic profile. Azaindole 32 was identified as a highly selective and orally available ROCK inhibitor able to cause a sustained blood pressure reduction in vivo.

AB - Rho kinase plays a pivotal role in several cellular processes such as vasoregulation, making it a suitable target for the treatment of hypertension and related disorders. We discovered a new compound class of Rho kinase (ROCK) inhibitors containing a 7-azaindole hinge-binding scaffold tethered to an aminopyrimidine core. Herein we describe the structure-activity relationships elucidated through biochemical and functional assays. The introduction of suitable substituents at the 3-position of the bicyclic moiety led to an increase in activity, which was required to design compounds with favorable pharmacokinetic profile. Azaindole 32 was identified as a highly selective and orally available ROCK inhibitor able to cause a sustained blood pressure reduction in vivo.

M3 - SCORING: Zeitschriftenaufsatz

VL - 3

SP - 1893

EP - 1904

JO - CHEMMEDCHEM

JF - CHEMMEDCHEM

SN - 1860-7179

IS - 12

M1 - 12

ER -