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Vol. 25 No. 11 (2013): Vol 25 Issue 11

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Synthesis, Characterization and Pharmacological Evaluation of N-Substituted Derivatives of 5-(4-Nitrophenyl)-1,3,4-oxadiazole-2yl-2"-sulphanyl Acetamide

https://doi.org/10.14233/ajchem.2013.14333
Samreen Gul
Department of Chemistry, Government College University, Lahore-54000, Pakistan
Aziz-ur Rehman
Department of Chemistry, Government College University, Lahore-54000, Pakistan
Muhammad Athar Abbasi
Department of Chemistry, Government College University, Lahore-54000, Pakistan
Khadija Nafeesa
Department of Chemistry, Government College University, Lahore-54000, Pakistan
Abdul Malik
HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan
Muhammad Ashraf
Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan
Tayaba Ismail
Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan
Irshad Ahmad
Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan

Corresponding Author(s) : Aziz-ur Rehman

azizryk@yahoo.com

Asian Journal of Chemistry, Vol. 25 No. 11 (2013): Vol 25 Issue 11

Abstract

A series of new N-substituted 5-(4-nitrophenyl)-1,3,4-oxadiazole-2-yl-2"-sulphanyl acetamides was synthesized and enzyme inhibiting activity was screened for all these chemical entities. Structural characterization of all these compounds was made by IR, EI-MS and 1H NMR. All derivatives demonstrated different extent of activity for lipoxygenase (LOX), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Compounds 6j exhibited excellent lipoxygenase inhibitory potential but against acetylcholinesterase the inhibitory potential is not appreciable and it is inactive against butyrylcholinesterase. Similarly compound 6e have good inhibitory potential against lipoxygenase with IC50 value 50.41 ± 0.12 μM while for acetylcholinesterase IC50 value is 174.21 ± 0.11 μM and 6e does not show any inhibitory potential for butyrylcholinesterase. Compound 6o showed good inhibition against acetylcholinesterase and butyrylcholinesterase but for lipoxygenase its inhibitory activity is the least.

Keywords

4-Nitrobenzoic acids Oxadiazoles Cholinesterase Lipoxygenase 1H NMR and EI-MS
Gul, S., Rehman, A.- ur, Athar Abbasi, M., Nafeesa, K., Malik, A., Ashraf, M., … Ahmad, I. (2013). Synthesis, Characterization and Pharmacological Evaluation of N-Substituted Derivatives of 5-(4-Nitrophenyl)-1,3,4-oxadiazole-2yl-2"-sulphanyl Acetamide. Asian Journal of Chemistry, 25(11), 6231–6236. https://doi.org/10.14233/ajchem.2013.14333
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