Abstract
We describe design, syntheses and structure-activity relationships of a novel class of 4,6-disubstituted quinazoline glucokinase activators. Prototype quinazoline leads (4 and 5) were designed based on the X-ray analyses of the previous 2-aminobenzamide lead classes. Modifications of the quinazoline leads led to the identification of a potent GK activator (21d).
MeSH terms
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Animals
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Blood Glucose / analysis
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Drug Discovery
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Glucokinase / chemistry*
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Glucokinase / metabolism
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / chemistry*
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Hypoglycemic Agents / pharmacology
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Mice
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Quinazolines / chemical synthesis
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Quinazolines / chemistry*
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Quinazolines / pharmacology
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Blood Glucose
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Hypoglycemic Agents
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Quinazolines
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Glucokinase