Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 19, Issue 1, Pages 384-392Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.11.016
Keywords
Heterocyclic homoprostanoids; Anti-inflammatory activity; Bovine serum albumin; Myeloperoxidase assay; DPP-IV inhibition; Oral glucose tolerance test; Diclofenac
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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 IC(50) 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. (C) 2010 Elsevier Ltd. All rights reserved.
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