Abstract
Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and –NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.
Keywords: N-substituted TZDs, antidiabetic, anticancer, anti-inflammatory, aldose reductase activity, alkonic acid.
Mini-Reviews in Medicinal Chemistry
Title:Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions
Volume: 19 Issue: 4
Author(s): Rakesh Gupta, Hardik Joshi and C.S. Ramaa*
Affiliation:
- Department of Pharmaceutical Chemistry, Bharati Vidyapeeth's College of Pharmacy, Navi-Mumbai,India
Keywords: N-substituted TZDs, antidiabetic, anticancer, anti-inflammatory, aldose reductase activity, alkonic acid.
Abstract: Thiazolidine-2,4-dione (TZD) is one of the most frequently encountered heterocyclic rings which has been implicated in design and synthesis of entities for various pathogenic conditions including cancer. Since its discovery various substitutions at 5th position have been carried out and reviewed. Various substitutions at 5th position have led to generation of glitazones, whose target peroxisome proliferating activated receptor γ (PPARγ) was found decade after their discovery. Acidic hydrogen (-NH) of TZD is a prime pharmacophoric requirement for the activation of PPARγ. However, advanced in-silico techniques have helped to design compounds bearing substitutions at both methylene and –NH group of TZD, targeting range of enzymes involved in various pathological conditions viz., diabetes, hyperlipidemia, infectious disease, inflammation and cancer. The promising activities shown by methylene and N-substituted TZDs in above mentioned therapeutic areas, prompted us to collate the information which would help researchers to alter the structure of existing ligands and to design new TZD derivatives with better safety and efficacy profiles.
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Cite this article as:
Gupta Rakesh , Joshi Hardik and Ramaa C.S. *, Assorted Applications of N-substituted-2,4-thiazolidinediones in Various Pathological Conditions, Mini-Reviews in Medicinal Chemistry 2019; 19 (4) . https://dx.doi.org/10.2174/1389557518666171129163426
DOI https://dx.doi.org/10.2174/1389557518666171129163426 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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