Discovery and optimization of indole and 7-azaindoles as Rho kinase (ROCK) inhibitors (Part-II)
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 scaff...
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Published in | Bioorganic & medicinal chemistry letters Vol. 21; no. 23; pp. 7113 - 7118 |
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Main Authors | , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Amsterdam
Elsevier Ltd
01.12.2011
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 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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Bibliography: | http://dx.doi.org/10.1016/j.bmcl.2011.09.084 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23 ObjectType-Article-2 ObjectType-Feature-1 |
ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2011.09.084 |