Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents

Thiazolidinediones are well known for causing reduction in blood glucose levels. A number of thiazolidinediones have been approved for clinical use in diabetes. Present research work is based on the synthesis of thiazolidinedione derivatives that were designed previously using 2D QSAR for antidiabet...

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Main Authors: Prasanna A. Datar, Sainath B. Aher
Format: Article
Language:English
Published: Elsevier 2016-09-01
Series:Journal of Saudi Chemical Society
Subjects:
Online Access:http://www.sciencedirect.com/science/article/pii/S1319610312001615
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author Prasanna A. Datar
Sainath B. Aher
author_facet Prasanna A. Datar
Sainath B. Aher
author_sort Prasanna A. Datar
collection DOAJ
description Thiazolidinediones are well known for causing reduction in blood glucose levels. A number of thiazolidinediones have been approved for clinical use in diabetes. Present research work is based on the synthesis of thiazolidinedione derivatives that were designed previously using 2D QSAR for antidiabetic activity. Thiazolidine-2,4-diones derivatives having carboxylic ester appendages at N-3 and 5-substituted benzylidene were studied and the syntheses of only four derivatives were performed that were predicted to have promising antidiabetic activities. Their effect on hypoglycemic activity was performed using a sucrose loaded model. Compounds 5a and 5b were found to have prominent activities at 100 mg/kg by oral route administration.
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spelling doaj.art-6dd2fbb15a8b4ca1bccdb52c99a4853f2022-12-21T21:58:00ZengElsevierJournal of Saudi Chemical Society1319-61032016-09-0120S1S196S20110.1016/j.jscs.2012.10.010Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agentsPrasanna A. DatarSainath B. AherThiazolidinediones are well known for causing reduction in blood glucose levels. A number of thiazolidinediones have been approved for clinical use in diabetes. Present research work is based on the synthesis of thiazolidinedione derivatives that were designed previously using 2D QSAR for antidiabetic activity. Thiazolidine-2,4-diones derivatives having carboxylic ester appendages at N-3 and 5-substituted benzylidene were studied and the syntheses of only four derivatives were performed that were predicted to have promising antidiabetic activities. Their effect on hypoglycemic activity was performed using a sucrose loaded model. Compounds 5a and 5b were found to have prominent activities at 100 mg/kg by oral route administration.http://www.sciencedirect.com/science/article/pii/S13196103120016152D QSARMLRHypoglycemic activityThiazolidinedionesDiabetesSucrose loaded model (SLM)
spellingShingle Prasanna A. Datar
Sainath B. Aher
Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
Journal of Saudi Chemical Society
2D QSAR
MLR
Hypoglycemic activity
Thiazolidinediones
Diabetes
Sucrose loaded model (SLM)
title Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
title_full Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
title_fullStr Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
title_full_unstemmed Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
title_short Design and synthesis of novel thiazolidine-2,4-diones as hypoglycemic agents
title_sort design and synthesis of novel thiazolidine 2 4 diones as hypoglycemic agents
topic 2D QSAR
MLR
Hypoglycemic activity
Thiazolidinediones
Diabetes
Sucrose loaded model (SLM)
url http://www.sciencedirect.com/science/article/pii/S1319610312001615
work_keys_str_mv AT prasannaadatar designandsynthesisofnovelthiazolidine24dionesashypoglycemicagents
AT sainathbaher designandsynthesisofnovelthiazolidine24dionesashypoglycemicagents