462619-75-6Relevant academic research and scientific papers
Synthesis of some new N-substituted-N-(2,3-Dihydro-[1,4]benzodioxin-6-yl)-4-acetamidobenzenesulfonamides as valuable antibacterial agents
Abbasi,Tariq,Aziz-Ur-Rehman,Siddiqui,Ahmad,Malik,Shah
, p. 198 - 209 (2016)
The aim of the research was to investigate the anti-bacterial potential of some N-substituted sulfonamides bearing benzodioxane moiety. The synthesis was started by reaction of N-2,3-dihydrobenzo[1,4]dioxin-6-amine with 4-acetamidobenzene-1-sulfonyl chloride in the presence of 10% aqueous Na2CO3 solution to yield N-(2,3-dihydrobenzo[1,4]-dioxin-6-yl)-4-acetamidobenzenesulfonamide, which was further reacted with alkyl/aralkyl halides in DMF and lithium hydride as a base to afford N-substituted-N-(2,3dihydro-[1,4]-benzodioxin-6-yl)-4-acetamidobenzenesulfonamides. All the synthesized compounds were characterized by spectral data (IR, 1H NMR, EI-MS, and HR-MS). The compounds were tested for antibacterial activity and most of them exhibited potent therapeutic potential against various Gram-negative and Gram-positive strains.
Synthesis, characterization and biological screening of some new sulfonamides derivatives of 1,4-benzodioxane-6-amine
Irshad, Misbah,Abbasi, Muhammad Athar,Rehman, Aziz-Ur,Siddiqui, Sabahat Zahra,Ashraf, Muhammad,Ejaz, Syeda Abida,Lodhi, Muhammad Arif,Jamal, Syed Babar
, p. 660 - 673 (2014/12/11)
In the present study, a series of N-substituted derivatives of 1,4-benzodioxane-6-amine have been synthesized. The reaction of 1,4-benzodioxane-6-amine (1) with various alkyl/aryl sulfonyl chlorides (2a-k) yielded N-alkyl/aryl sulfonamides (3a-k), which further on treatment with benzyl chloride (4) in the presence of sodium hydride furnished into N-benzylated sulfonamides (6a-k) while the reaction of 3a-k with ethyl iodide (5 ) yielded N-ethylated sulfonamides 7a-k. These derivatives were characterized by IR, 1H-NMR and EI-MS and then screened against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase (LOX) enzymes and were found to be good inhibitors of lipoxygenase only. The interaction between inhibitors and target enzymes were computationally observed which correlates with the experimental results.
