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Biological activity of synthesized 5-{1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl}-2-mercapto-1,3,4-oxadiazole derivatives demonstrated by in silico and BSA binding studies BJPS
Iqbal,Javed; Rehman,Aziz-ur-; Abbasi,Muhammad Athar; Siddiqui,Sabahat Zahra; Rasool,Shahid; Ashraf,Muhammad; Iqbal,Ambar; Hamid,Sujhla; Chohan,Tahir Ali; Khalid,Hira; Laulloo,Sabina Jhaumeer; Shah,Syed Adnan Ali.
We synthesized a series of compounds bearing pharmacologically important 1,3,4-oxadiazole and piperidine moieties. Spectral data analysis by 1H-NMR, 13C-NMR, IR and EI-MS was used to elucidate the structures of the synthesized molecules. Docking studies explained the different types of interaction of the compounds with amino acids, while bovine serum albumin (BSA) binding interactions showed their pharmacological effectiveness. Antibacterial screening of these compounds demonstrated moderate to strong activity against Salmonella typhi and Bacillus subtilis but only weak to moderate activity against the other three bacterial strains tested. Seven compounds were the most active members as acetyl cholinesterase inhibitors. All the compounds presented...
Tipo: Info:eu-repo/semantics/article Palavras-chave: 1; 3; 4-Oxadiazole Acetylcholinesterase (AChE) inhibition Antibacterial activity Piperidine Sulfonamide Urease inhibition.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100596
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Synthesis of new 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl) sulfonyl]amino}-N-(un/substituted-phenyl)acetamides as α-glucosidase and acetylcholinesterase inhibitors and their in silico study BJPS
Abbasi,Muhammad Athar; Riaz,Sajid; Rehman,Aziz-ur-; Siddiqui,Sabahat Zahra; Shah,Syed Adnan Ali; Ashraf,Muhammad; Lodhi,Muhammad Arif; Khan,Farman Ali.
The aim of the present research work was to investigate the enzyme inhibitory potential of some new sulfonamides having benzodioxane and acetamide moieties. The synthesis was started by the reaction of N-2,3-dihydrobenzo[1,4]-dioxin-6-amine (1) with 4-methylbenzenesulfonyl chloride (2) in the presence of 10% aqueous Na2CO3 to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-methylbenzenesulfonamide (3), which was then reacted with 2-bromo-N-(un/substituted-phenyl)acetamides (6a-l) in DMF and lithium hydride as a base to afford various 2-{2,3-dihydro-1,4-benzodioxin-6-yl[(4-methylphenyl)sulfonyl]amino}-N-(un/substituted-phenyl)acetamides (7a-l). All the synthesized compounds were characterized by their IR and 1H-NMR spectral data along with CHN analysis data....
Tipo: Info:eu-repo/semantics/article Palavras-chave: Benzodioxane; Acetamide; Spectral analysis; A-Glucosidase; Acetylcholinesterase; Molecular docking.
Ano: 2019 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502019000100518
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