Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives

Reddy, Manohara SA and Mudgal, Jayesh and Bansal, Punit and Vasantharaju, SG and Srinivasan, KK and Rao, Mallikarjuna C and Kutty, Gopalan N (2011) Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives. Bioorganic & Medicinal Chemistry, 19. pp. 384-392. ISSN 0968-0896

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A series of 19 heterocyclic homoprostanoids were synthesized from easily available oleic and ricinoleic acids and evaluated for their possible antioxidant, anti-inflammatory and anti-hyperlipidaemic activities. Compounds with thioxo- and oxoimidazole ring (1) and (2) have shown potent antioxidant activity with IC50 values 0.23 ± 0.09 and 0.41 ± 0.01 mM comparable with standard ascorbic acid. Compound (3) with a quinoxaline ring showed maximum inhibition of BSA denaturation at 1 mM concentration and comparable with standard diclofenac. Incorporation of electron withdrawing substitutions like chloro- and nitrogroups in the quinoxaline ring has resulted in an increase anti-inflammatory activity. Test compounds (3), (3a) and (3c) showed modest inhibition of DPP-IV in vitro. However, the unsubstituted quinoxaline (3) and substituted quinoxalines (3b and 3c) reduced plasma glucose levels indicating the presence of hypoglycemic activity.

Item Type: Article
Uncontrolled Keywords: Heterocyclic homoprostanoids,Anti-inflammatory activity ,Bovine serum albumin, Myeloperoxidase assay ,DPP-IV inhibition , Oral glucose tolerance test Diclofenac.
Subjects: Pharmacy > MCOPS Manipal > Pharmaceutical Chemistry
Pharmacy > MCOPS Manipal > Pharmaceutical Quality Assurance
Pharmacy > MCOPS Manipal > Pharmacology
Depositing User: KMC Manipal
Date Deposited: 23 Jan 2012 04:20
Last Modified: 22 Oct 2013 11:03

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