Abstract |
The promising activity shown by compounds containing thiazolidine-2,4-dione nucleus in numerous categories such as anti-hyperglycaemics, aldose reductase inhibitors, anti- cancer, anti-inflammatory, anti-arthritics, anti-microbials, etc. has made it an indispensable anchor for development of new therapeutic agents. Varied substituents on the thiazolidine-2,4-dione nucleus have provided a wide spectrum of biological activities. Importance of this nucleus in some activities like, peroxisome proliferator activated receptor γ (PPARγ) agonism and PPARγ-dependent and -independent anti- cancer activities are reviewed separately in literature. Short reviews on biological importance of this nucleus are also known in literature. However, owing to fast development of new drugs possessing thiazolidine-2,4-dione nucleus many research reports are generated in short span of time. So, there is a need to couple the latest information with the earlier information to understand the current status of thiazolidine-2,4-dione nucleus in medicinal chemistry research. In the present review, various derivatives of thiazolidine-2,4-diones with different pharmacological activities are described on the basis of substitution pattern around the nucleus combined with the docking studies performed in the active site of the corresponding receptors with an aim to help medicinal chemists for developing an SAR on thiazolidine-2,4-dione derived compounds for each activity. This discussion will further help in the development of novel thiazolidine-2,4-dione compounds.
|
Authors | Viral S Jain, Dhagash K Vora, C S Ramaa |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 21
Issue 7
Pg. 1599-620
(Apr 01 2013)
ISSN: 1464-3391 [Electronic] England |
PMID | 23419324
(Publication Type: Journal Article, Review)
|
Copyright | Copyright © 2013 Elsevier Ltd. All rights reserved. |
Chemical References |
- Anti-Infective Agents
- Anti-Inflammatory Agents
- Antineoplastic Agents
- Enzyme Inhibitors
- Hypoglycemic Agents
- PPAR gamma
- Thiazolidinediones
- thiazolidine-2,4-dione
|
Topics |
- Animals
- Anti-Infective Agents
(chemistry, pharmacology)
- Anti-Inflammatory Agents
(chemistry, pharmacology)
- Antineoplastic Agents
(chemistry, pharmacology)
- Arthritis, Rheumatoid
(drug therapy)
- Bacterial Infections
(drug therapy)
- Drug Design
- Enzyme Inhibitors
(chemistry, pharmacology)
- Humans
- Hyperglycemia
(drug therapy)
- Hypoglycemic Agents
(chemistry, pharmacology)
- Mycoses
(drug therapy)
- Neoplasms
(drug therapy, metabolism)
- PPAR gamma
(agonists, chemistry, metabolism)
- Structure-Activity Relationship
- Thiazolidinediones
(chemistry, pharmacology)
|