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Divekar, Kalpana
- Synthesis and Characterization of Some New Oxadiazole Derivatives as Antiinflammatory Agents
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Authors
Affiliations
1 College of Pharmaceutical Sciences, DSU, Bengaluru, Karnataka, IN
1 College of Pharmaceutical Sciences, DSU, Bengaluru, Karnataka, IN
Source
Research Journal of Pharmacy and Technology, Vol 12, No 5 (2019), Pagination: 2416-2420Abstract
Oxadiazoles have impacted numerous areas of drug discovery like muscarinic antagonists, benzodiazepines receptor partial agonists, dopamine transporters, antirhinovirals, growth hormone secretagogues, 5-HT antagonists, antispasmodics, nematocidals, fungicidal and microbicides, analgesics, anti-inflammatory, anticonvulsant, antibacterial, immunosuppressants, antiplatelet and antithrombics. Oxadiazoles are known to be bio-isosters for amide and esters. Due to a good metabolic stability oxadiazole ring exhibits an improved pharmacokinetic and in-vivo performance. Owing to this property this heterocyclic ring is considered as an important structural motif for the pharmaceutical Industry. In the present work, an attempt was made to synthesize some novel oxadiazole derivatives by converting the Aromatic carboxylic acids into acid esters by conventional esterification. The esters obtained were treated with hydrazine hydrate to give aromatic hydrazides. Those hydrazides on refluxing with carbon di sulfide in presence of potassium hydroxide yielded different oxadiazole derivatives. Then those oxadiazole derivatives were subjected to acetylation and aromatic group attachment. The synthesized compounds were characterized and confirmed by IR and 1HNMR spectroscopy and then screened for antiinflammatory activity. The anti-inflammatory activity of newly synthesized oxadiazole derivatives were carried out by the carrageenan induced rat hind paw edema method using Diclofenac sodium as standard. Among the twelve newly synthesized oxadiazole derivatives ten compounds showed considerable activity comparable with standard.Keywords
Bioisosters, Oxadiazoles, Anticonvulsants.
References
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- The Hypoglycemic and Hypolipidemic Effect of 5- Naphthalidin-2, 4 Thiazolidinedione Derivatives in Alloxan Induced Type Ii Diabetic Model
Abstract Views :143 |
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Authors
Affiliations
1 Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Dayananda Sagar University, Bangalore, Karnataka, IN
2 Department of Pharmaceutics, Dr. Ravi Patil College of Pharmacy, Belgaum, Karnataka,, IN
1 Department of Pharmaceutical Chemistry, College of Pharmaceutical Sciences, Dayananda Sagar University, Bangalore, Karnataka, IN
2 Department of Pharmaceutics, Dr. Ravi Patil College of Pharmacy, Belgaum, Karnataka,, IN
Source
Research Journal of Pharmacy and Technology, Vol 15, No 4 (2022), Pagination: 1505-1511Abstract
Objective: The present study was undertaken to study antidiabetic and antihyperlipidemic potentials of 5- naphthalidin-2, 4-thiazolidinediones derivatives and its interaction with rosiglitazone in alloxan-induced diabetic rats. Methods: Diabetes was induced in male swiss albino rats by single intramuscular injection of alloxan (0.15 mg/Kg i.m) and NIDDM-rats received 4b, 4c or 4d (36 mg/Kg, p.o). Fasting blood glucose (FBG) levels were measured by glucose-oxidase & peroxidase reactive strips. Serum biochemical parameters such as total cholesterol (TC), triglycerides (TG), very low density lipoprotein (VLDL), low density lipoprotein (LDL) and high density lipoprotein (HDL) cholesterol were estimated. The statistical analysis of results was carried out using Student t-test and one-way analysis (ANOVA) followed by Duncan's Multiple Range Test (DMRT). Results: The results revealed that 4b, 4c and 4d showed promising results by lowering the blood glucose. Moreover, 4c compound displayed high efficiency for lowering lipid profiles compared to others. Conclusion: These results suggest that taking 5- naphthalidin-2, 4 TZD orally twice/day is a valuable treatment for Non insulin dependent diabetes mellitus (NIDDM) and hypolipidemic agent. They exert their effects through altering regulation genes in glucose and lipid metabolisms in diabetic rats.Keywords
Diabetes, Free radical scavenging activity, RIN-5F cells, Diseased human lung fibroblast.References
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