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Peer-reviewed veterinary case report

Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2009
Authors:
Ho, Koc-Kan et al.
Affiliation:
Ligand Pharmaceuticals · United States
Species:
rodent

Abstract

The profile of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are consistent with the observed SAR. Compounds from the series are potent in a cell migration assay and possess a favorable kinase selectivity. In vivo activity was demonstrated for compound 1A in a spontaneous hypertensive rat model.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/19800787/