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. 2018 Aug 15;28(15):2622-2626.
doi: 10.1016/j.bmcl.2018.06.040. Epub 2018 Jun 19.

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors

Upul K Bandarage  1 , Jingrong Cao  2 , Jon H Come  2 , John J Court  2 , Huai Gao  2 , Marc D Jacobs  2 , Craig Marhefka  2 , Suganthi Nanthakumar  2 , Jeremy Green  3
Affiliations

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors

Upul K Bandarage et al. Bioorg Med Chem Lett. .

Abstract

Rho kinase (ROCK) inhibitors are potential therapeutic agents for the treatment of a variety of disorders including hypertension, glaucoma and erectile dysfunction. Here we disclose a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Substitution of the 3-position of 7-azaindole led to compounds such as 37, which possess excellent ROCK inhibitory potency and high selectivity against the closely related kinase PKA.

Keywords: 7-Azaindole; Lipophilic efficiency; ROCK; Rho kinase; Solubilizing group; Structure-based design.

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