Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372165 | Bioorganic & Medicinal Chemistry Letters | 2011 | 6 Pages |
Abstract
Therapeutic interventions with Rho kinase (ROCK) inhibitors may effectively treat several disorders such as hypertension, stroke, cancer, and glaucoma. Herein we disclose the optimization and biological evaluation of potent novel ROCK inhibitors based on substituted indole and 7-azaindole core scaffolds. Substitutions on the indole C3 position and on the indole NH and/or amide NH positions all yielded potent and selective ROCK inhibitors (25, 42, and 50). Improvement of aqueous solubility and tailoring of in vitro and in vivo DMPK properties could be achieved through these substitutions.
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Related Topics
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Organic Chemistry
Authors
E. Hampton Sessions, Sarwat Chowdhury, Yan Yin, Jennifer R. Pocas, Wayne Grant, Thomas Schröter, Li Lin, Claudia Ruiz, Michael D. Cameron, Philip LoGrasso, Thomas D. Bannister, Yangbo Feng,