Synthesis of some new biologically active N-substituted-2''- [[phenylsulfonyl][piperidin-1-yl]amino]acetamide derivatives
Pakistan Journal of Pharmaceutical Sciences. 2014; 27 (3): 517-524
in English
| IMEMR
| ID: emr-142168
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.
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Index:
IMEMR (Eastern Mediterranean)
Main subject:
Acetylcholinesterase
/
Sulfones
/
Butyrylcholinesterase
/
Lipoxygenase
/
Acetamides
Language:
English
Journal:
Pak. J. Pharm. Sci.
Year:
2014
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