title: Synthesis of some new biologically active N-substituted-2''- [(phenylsulfonyl)(piperidin-1-yl)amino]acetamide derivatives.
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 N-substituted derivatives of acetamide (7a-k) bearing piperidine moiety. All the synthesized compounds were confirmed on the basis of IR, EIMS and (1)H-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.
authors.affiliation: Department of Chemistry, Government College University, Lahore, Pakistan.
authors.forename: Hira
authors.initials: H
authors.lastname: Khalid
authors.affiliation: Department of Chemistry, Government College University, Lahore, Pakistan.
authors.forename: Aziz-Ur
authors.initials: AU
authors.lastname: Rehman
authors.affiliation: Department of Chemistry, Government College University, Lahore, Pakistan.
authors.forename: Muhammad Athar
authors.initials: MA
authors.lastname: Abbasi
authors.affiliation: Department of Chemistry, Government College University, Lahore, Pakistan.
authors.forename: Sabahat Zahra
authors.initials: SZ
authors.lastname: Siddiqui
authors.affiliation: HEJ Research Institute of Chemistry, ICCBS, University of Karachi, Karachi, Pakistan.
authors.forename: Abdul
authors.initials: A
authors.lastname: Malik
authors.affiliation: Department of Biochemistry and Biotechnology, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
authors.forename: Muhammad
authors.initials: M
authors.lastname: Ashraf
authors.affiliation: Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
authors.forename: Irshad
authors.initials: I
authors.lastname: Ahmad
authors.affiliation: Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
authors.forename: Syeda Abida
authors.initials: SA
authors.lastname: Ejaz
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D000110:Acetylcholinesterase / Q000378:metabolism; D002091:Butyrylcholinesterase / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D016859:Lipoxygenase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D002800:Cholinesterase Inhibitors; D016859:Lipoxygenase Inhibitors; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase