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Bioorg Chem ; 45: 12-28, 2012 Dec.
Article in English | MEDLINE | ID: mdl-23064124

ABSTRACT

We report a series of new glitazones incorporated with phenylalanine and tyrosine. All the compounds were tested for their in vitro glucose uptake activity using rat-hemidiaphragm, both in presence and absence of insulin. Six of the most active compounds from the in vitro screening were taken forward for their in vivo triglyceride and glucose lowering activity against dexamethazone induced hyperlipidemia and insulin resistance in Wistar rats. The liver samples of rats that received the most active compounds, 23 and 24, in the in vivo studies, were subjected to histopathological examination to assess their short term hepatotoxicity. The investigations on the in vitro glucose uptake, in vivo triglyceride and glucose lowering activity are described here along with the quantitative structure-activity relationships.


Subject(s)
Hypoglycemic Agents/chemical synthesis , Phenylalanine/chemistry , Thiazolidinediones/chemistry , Tyrosine/chemistry , Animals , Blood Glucose/drug effects , Blood Glucose/metabolism , Drug Evaluation, Preclinical , Hyperlipidemias/chemically induced , Hyperlipidemias/drug therapy , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Liver/drug effects , Liver/pathology , Rats , Rats, Wistar , Structure-Activity Relationship , Thiazolidinediones/chemical synthesis , Triglycerides/blood
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