Abstract
A series of substituted pyridines and purines containing 2,4-thiazolidinedione were designed and synthesized from their corresponding pyridines and purines. These synthesized compounds (entry no. 6a-d, 12a-e, 18a-d, 23a-c) were evaluated for their effect on triglyceride accumulation in 3T3-L1 cells in vitro and their hypoglycemic and hypolipidemic activity in the genetically diabetic KKA(y) mice in vivo. On the basis of their biological activities, 5-(4-[2-[N-methyl-(5-phenyl-pyridin-2-yl)amino]ethoxy]benzyl)thiazolidine-2,4-dione (6d) was selected as a candidate for further pharmacological studies.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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3T3-L1 Cells
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Animals
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Blood Glucose / drug effects
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Cell Division / drug effects
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Cells, Cultured
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Diabetes Mellitus, Experimental / drug therapy*
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Disease Models, Animal
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Drug Design
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Hepatocytes / drug effects
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Hepatocytes / metabolism
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Hypoglycemic Agents / administration & dosage
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Hypoglycemic Agents / therapeutic use
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Hypolipidemic Agents / administration & dosage
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Hypolipidemic Agents / therapeutic use
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Male
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Mice
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Molecular Structure
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Purines / chemical synthesis*
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Purines / pharmacology*
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Pyridines / chemical synthesis*
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Pyridines / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Thiazolidinediones / chemistry*
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Triglycerides / metabolism
Substances
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Blood Glucose
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Hypoglycemic Agents
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Hypolipidemic Agents
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Purines
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Pyridines
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Thiazolidinediones
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Triglycerides
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2,4-thiazolidinedione