Author/Authors :
Khalid, Hira Government College University - Department of Chemistry, Pakistan , Aziz-ur-Rehman Government College University - Department of Chemistry, Pakistan , Abbasi, Muhammad Athar Government College University - Department of Chemistry, Pakistan , Siddiqui, Sabahat Zahra Government College University - Department of Chemistry, Pakistan , Abdul Malik University of Karachi - ICCBS, HEJ Research Institute of Chemistry, Pakistan , Ashraf, Muhammad Islamia University of Bahawalpur - Department of Biochemistry and Biotechnology, Pakistan , Ahmad, Irshad Islamia University of Bahawalpur - Department of Pharmacy, Pakistan , Ejaz, Abida Islamia University of Bahawalpur - Department of Pharmacy, Pakistan
Abstract :
A new series of N-aryl/aralkyl substitued-2-[(phenylsulfonyl)(piperidin-1-yl)amino]acetamide (7a-k) was synthesized. These derivatives were geared up by the pairing of benzenesulfonyl chloride (4) with 1-aminopiperidine (5) under dynamic pH control in aqueous media to afford parent compound N-(Piperidin-1-yl) benzenesulfonamide (6), followed by the substitution at nitrogen atom with different electrophiles N-aryl/aralkyl-substituted-2-bromoacetamides (3a-k) in the presence of sodium hydride (NaH) and N,N-Dimethylformamide (DMF) to give a new series of Nsubstituted derivatives of acetamide (7a-k) bearing piperidine moiety. All the synthesized compounds were confirmed on the basis of IR, EIMS and 1H-NMR spectral data. The synthesized compounds were evaluated against acetylcholinesterase and butyrylcholinesterase (AChE and BChE) respectively and lipoxygenase (LOX) enzymes. Almost all the synthesized compounds displayed promising activity but few of them remained inactive against lipoxygenase enzymes.
Keywords :
1 , Aminopiperidine , benzenesulfonyl chloride , acetamide , butyrylcholinesterase , spectral characterization.
