Muhammad A Abbasi1 
,
Saima Najm1,
Aziz-ur-Rehman .1,
Shahid Rasool1,
Khalid M Khan2,
Muhammad Ashraf3,
Rumana Nasar3,
Umber Alam3
For correspondence:- Muhammad Abbasi Email: atrabbasi@yahoo.com Tel:+9242111000010
Received: 6 January 2014 Revised: 14 November 2014 Published: 30 January 2015
Citation: Abbasi MA, Najm S, . A, Rasool S, Khan KM, Ashraf M, et al. Evaluation of sulfonamide derivatives of dagenan chloride as lipoxygenase and ^5;-glucosidase inhibitors. Trop J Pharm Res 2015; 14(1):47-54 doi: 10.4314/tjpr.v14i1.8
© 2015 The authors.
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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 (1H-NMR) 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.
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