Synthesis, enzyme inhibition and molecular docking studies of 1- Arylsulfonyl-4-phenylpiperazine derivatives | [Pakistan Journal of Pharmaceutical Sciences • 2017]

Author(s):

1. Muhammad Athar Abbasi: Department of Chemistry, Government College University,Lahore,Pakistan

2. Ambreen Anwar: Department of Chemistry, Government College University,Lahore,Pakistan

3. Aziz-ur-Rehman: Department of Chemistry, Government College University,Lahore,Pakistan

4. Sabahat Zahra Siddiqui: Department of Chemistry, Government College University,Lahore,Pakistan

5. Kaniz Rubab: Department of Chemistry, Government College University,Lahore,Pakistan

6. Syed Adnan Ali Shah: Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia; Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Level 9, FF3, Universiti Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia

7. Muhammad Arif Lodhi: Department of Biochemistry, Abdul Wali Khan University,Mardan,Pakistan

8. Farman Ali Khan: Department of Biochemistry, Abdul Wali Khan University,Mardan,Pakistan

9. Muhammad Ashraf: Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

10. Umber Alam: Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

Abstract:

Heterocyclic molecules have been frequently investigated to possess various biological activities during the last few decades. The present work elaborates the synthesis and enzymatic inhibition potentials of a series of sulfonamides. A series of 1-arylsulfonyl-4-Phenylpiperazine (3a-n) geared up by the reaction of 1-phenylpiperazine (1) and different (un)substituted alkyl/arylsulfonyl chlorides (2a-n), under defined pH control using water as a reaction medium. The synthesized molecules were characterized by 1H-NMR, 13C-NMR, IR and EI-MS spectral data. The enzyme inhibition study was carried on a-glucosidase, lipoxygenase (LOX), acetyl cholinesterase (AChE) and butyryl cholinesterase (BChE) enzymes supported by docking simulation studies and the IC50 values rendered a few of the synthesized molecules as moderate inhibitors of these enzymes where, the compound 3e exhibited comparatively better potency against a-glucosidase enzyme. The synthesized compounds showed weak or no inhibition against LOX, AChE and BChE enzymes.

Page(s): 1715-1724

DOI: DOI not available

Published: Journal: Pakistan Journal of Pharmaceutical Sciences, Volume: 30, Issue: 5, Year: 2017

Keywords:

Phenylpiperazine , alkylarylsulfonyl chlorides , enzyme inhibition activity and spectral characterization

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