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Discovery of novel glitazones incorporated with phenylalanine and tyrosine: Synthesis, antidiabetic activity and structure-activity relationships

Kumar, Prashantha BR and Baig, Nasir R and Sudhir, Sai and Kar, Koyal and Kiranmai, M. and Pankaj, M and Joghee, Nanjan M (2012) Discovery of novel glitazones incorporated with phenylalanine and tyrosine: Synthesis, antidiabetic activity and structure-activity relationships. In: BIOORGANIC CHEMISTRY, 45 . pp. 12-28.

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Official URL: http://dx.doi.org/10.1016/j.bioorg.2012.08.002

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. (C) 2012 Elsevier Inc. All rights reserved.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to ACADEMIC PRESS INC ELSEVIER SCIENCE, USA
Keywords: CoMSIA;Dexamethazone;Glitazones;Glucose uptake activity;Insulin resistance;Thiazolidinediones
Department/Centre: Division of Chemical Sciences > Organic Chemistry
Depositing User: Francis Jayakanth
Date Deposited: 26 Feb 2013 12:20
Last Modified: 26 Feb 2013 12:20
URI: http://eprints.iisc.ac.in/id/eprint/45862

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