Abstract
A series of novel arylacetamides were designed to further explore the GK binding property at the aminothiazole C5 position. The C5-amide substituted aminothiazoles 7a-f generally displayed decreased potency, whereas most of the C5-triazole substituted aminothiazoles retained good GK potency. Triazole 15 with a hydroxyethyl side chain was the most potent among the current series possessing an EC50 value of 0.18 μM. Its R-enantiomer R-15 showed similar potency (0.22 μM) that deserves for further evaluation.
Original language | English (US) |
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Pages (from-to) | 531-535 |
Number of pages | 5 |
Journal | MedChemComm |
Volume | 2 |
Issue number | 6 |
DOIs | |
State | Published - Jun 2011 |
Externally published | Yes |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Pharmacology
- Pharmaceutical Science
- Drug Discovery
- Organic Chemistry