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Design, synthesis and biological evaluation of novel 5-(imidazolyl-methyl) thiazolidinediones as antidiabetic agents
- Source :
- Bioorganic chemistry. 115
- Publication Year :
- 2021
-
Abstract
- A newly designed series of imidazolyl-methyl- l-2,4-thiazolidinediones 9 (a-m) were synthesized and In Silico studies were carried out to rationalize their anti-diabetic activity. Generally, all newly synthesized thiazolidinediones had anti-hyperglycemic activity compared with a diabetic-control group, without toxicity in 3T3 cells (viability ≥ 90%). These studies revealed that the compounds 9e and 9b ( 11 ∗ 10 - 6 m o l / k g ) lowered blood glucose more effectively when compared to pioglitazone at the same dose. Following the administration of compound 9e, no weight gains or any serious side effects on liver and pancreas were observed. Moreover, the glucose consumption assay results showed a significant glucose-lowering effect (p
- Subjects :
- Male
medicine.drug_class
Cell Survival
Pharmacology
Biochemistry
Synthetic analogue
Diabetes Mellitus, Experimental
Mice
Structure-Activity Relationship
Diabetes mellitus
Catalytic Domain
Drug Discovery
medicine
Animals
Humans
Hypoglycemic Agents
Thiazolidinedione
Molecular Biology
Pancreas
Antidiabetic agents
Biological evaluation
Binding Sites
Pioglitazone
Chemistry
Organic Chemistry
3T3 Cells
medicine.disease
Rats
Molecular Docking Simulation
PPAR gamma
Glucose
Design synthesis
Liver
Drug Design
Toxicity
Thiazolidinediones
medicine.drug
Subjects
Details
- ISSN :
- 10902120
- Volume :
- 115
- Database :
- OpenAIRE
- Journal :
- Bioorganic chemistry
- Accession number :
- edsair.doi.dedup.....0c941ed0d484c559d7d2edb0fc7d8bc8