Antioxidant, anti-inflammatory and anti-hyperglycaemic activities of heterocyclic homoprostanoid derivatives |
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Authors: | Manohara Reddy S A Mudgal Jayesh Bansal Punit Vasanthraju S G Srinivasan K K Rao C Mallikarjuna Gopalan Kutty N |
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Institution: | a Department of Pharmacology, Manipal College of Pharmaceutical Sciences, Manipal University, Madhav Nagar, Manipal 576 104, Karnataka, India b Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal University, Madhav Nagar, Manipal 576 104, Karnataka, India c Department of Pharmaceutical Chemistry, Manipal College of Pharmaceutical Sciences, Manipal University, Madhav Nagar, Manipal 576 104, Karnataka, India |
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Abstract: | 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 nitro-groups 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. |
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Keywords: | Heterocyclic homoprostanoids Anti-inflammatory activity Bovine serum albumin Myeloperoxidase assay DPP-IV inhibition Oral glucose tolerance test Diclofenac |
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