Peer-reviewed veterinary case report
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model.
- Journal:
- Bioorganic & medicinal chemistry letters
- Year:
- 2015
- Authors:
- Thoma, Gebhard et al.
- Affiliation:
- Global Discovery Chemistry
- Species:
- rodent
Abstract
Design and optimization of benzo- and pyrido-thiazoles/isothiazoles are reported leading to the discovery of the potent, orally bioavailable Syk inhibitor 5, which was found to be active in a rat PK/PD model. Compound 5 showed acceptable overall kinase selectivity. However, in addition to Syk it also inhibited Aurora kinase in enzymatic and cellular settings leading to findings in the micronucleus assay. As a consequence, compound 5 was not further pursued.
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Search related cases →Original publication: https://pubmed.ncbi.nlm.nih.gov/26320624/