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

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

Ambreen Anwar Department of Chemistry, Government College University,Lahore,Pakistan

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

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

Kaniz Rubab Department of Chemistry, Government College University,Lahore,Pakistan

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

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

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

Muhammad Ashraf Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

Umber Alam Department of Chemistry, The Islamia University of Bahawalpur,Bahawalpur,Pakistan

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.