Synthesis of some new biologically active N-substituted-2''- [(phenylsulfonyl)(piperidin-1-yl)amino]acetamide derivatives.

Paper

Synthesis of some new biologically active N-substituted-2''- [(phenylsulfonyl)(piperidin-1-yl)amino]acetamide derivatives.

Published May 1, 2014 · H. Khalid, A. Rehman, M. Abbasi

Pakistan journal of pharmaceutical sciences

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2

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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.

Study Snapshot

New N-substituted-2'-[(phenylsulfonyl)(piperidin-1-yl)amino]acetamide derivatives show promising activity against acetylcholinesterase and butyrylcholinesterase enzymes, with some remaining inactive

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Synthesis of some new biologically active N-substituted-2''- [(phenylsulfonyl)(piperidin-1-yl)amino]acetamide derivatives.

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References

Synthesis, spectral analysis and biological screening of some new N-(un)substituted N-(5-chloro-2-methoxyphenyl)-aryl sulfonamides

New N-(5-chloro-2-methoxyphenyl)-aryl sulfonamides show moderate to good antibacterial activity, with structural changes in substituents significantly altering inhibitory properties.

Lipoxygenase inhibitory constituents from Periploca aphylla.

Bisflavan-3-ols 1, 2, and norterpenoid 3 show inhibitory potential against lipoxygenase, with IC(50) values ranging from 19.7 to 150.1 microM.

Protease inhibitors of the sulfonamide type: Anticancer, antiinflammatory, and antiviral agents

Sulfonamide derivatives show potential as anticancer, antiinflammatory, and antiviral agents, with potential applications in treating various diseases.

Cyclooxygenase, lipoxygenase and tumor angiogenesis

Arachidonate metabolites from the COX and 12-LOX pathways play a crucial role in regulating angiogenesis in tumor growth, with unanswered questions for future studies.

Acetylcholinesterase Mechanism of catalysis and inhibition

Acetylcholinesterase's catalytic power comes from polar solvation of the transition state by properly oriented dipoles, with the active site gorge playing a secondary role in substrate binding and inhibition.

Citations

Synthesis, Characterization And Biological Activities Of Sulfonamide Derivatives Bearing Piperidine Nucleus

This study synthesized 149 compounds with diverse pharmacological potential, including inhibitory potential against enzymes and antibacterial activity against various bacteria.