Article Sidebar
Published:
Feb 6, 2015DOI:
10.4314/tjpr.v14i1.8Keywords:
Article Details
Submission of a manuscript to this journal is a representation that the manuscript has not been published previously and is not under consideration for publication elsewhere.
All authors named in each manuscript would be required to sign a form (to be supplied by the Editor) so that they may retain their copyright in the article but to assign to us (the Publishers) and its licensees in perpetuity, in all forms, formats and media (whether known or created in the future) to (i) publish, reproduce, distribute, display and store the contribution, (ii) translate the contribution into other languages, create adaptations, reprints, include within collections and create summaries, extracts and/or abstracts of the contribution, (iii) create any other derivative works(s) based on the contribution, (iv) to exploit all subsidiary rights in the contribution, (v) the inclusion of electronic links from the contribution to third party material where-ever it may be located, and (vi) license any thrid party to do any or all of the above.
Main Article Content
Evaluation of Sulfonamide Derivatives of Dagenan Chloride as Lipoxygenase and α-Glucosidase Inhibitors
Abstract
Purpose: To study the enzyme inhibition activity of various sulfonamides derived from dagenan chloride.
Methods: The synthesis of N-(naphthalen-1-yl)-4-acetamidobenzenesulfonamide (3) was carried out by gearing up 1-naphthylamine (1) with dagenan chloride (2) in water in the presence of Na2CO3 solution. Further, compound 3 was treated with various alkyl/aralkyl halides (4a-o) to yield 5a-o in an aprotic polar solvent, DMF (dimethylformamide), using LiH as activator. The structures of all the synthesized molecules were corroborated by infra red spectroscopy (IR), proton nuclear magnetic resonance (1HNMR) and electron impact mass spectrometry (EI-MS) and screened against lipoxygenase and α- glucosidase using baicalein and acarbose as reference standards, respectively.
Results: Molecules 5e and 5j showed good lipoxygenase inhibition activity with IC50 (50 % inhibition concentration) value of 132.21 ± 0.73 and 133.33 ± 0.87 μmol/L, respectively, relative to reference, while 5m was the most active inhibitor of α-glucosidase with IC50 of 19.41 ± 0.55 μmol/L relative to reference.
Conclusion: Most of the synthesized compounds are good inhibitors of lipoxygenase but moderate inhibitors of α-glucosidase enzyme. These molecules should be evaluated for their in vivo activity to determine their potentials as anti-inflammatory and anti-diabetic drugs.
Keywords: 1-Naphthylamine, Sulfonamide, Lipoxygenase, α-Glucosidase, Dagenan chloride, Enzyme inhibitor, Anti-inflammatory, Anti-diabetic
