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Synthesis,biological screening and molecular docking studies of some ethylated sulfonamides having 1,4-Benzodioxane moiety
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نویسنده
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irshad m. ,abbasi m.a. ,aziz-ur-rehman a. ,siddiqui s.z. ,ali m.s. ,ashraf m. ,ismail t. ,ahmad i. ,hassan s. ,lodhi m.a. ,jamal s.b.
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منبع
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pakistan journal of pharmaceutical sciences - 2016 - دوره : 29 - شماره : 6 - صفحه:1913 -1925
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چکیده
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The presented study comprises the synthesis of a new series of ethylated sulfonamides in which 1,4- benzodioxane moietyhas been incorporated. the reaction of 1,4-benzodioxane-6-amine (1) with ethane sulfonyl chloride (2) yielded n-(2,3-dihydrobenzo[1,4]dioxin-6-yl)ethanesulfonamide (3),which further on treatment with various alkyl/aralkyl halides,4a-r,in n,n□-dimethylformamide (dmf) and in the presence of lithium hydride (lih) acting as a weak base and catalyst;yielded derivativesofn-alkyl/aralkyl substituted n-(2,3-dihydrobenzo[1,4]dioxin-6- yl)ethanesulfonamides (5a-r). the characterization of these derivatives was carried out by different spectroscopic techniques like infra red,proton-nmr and mass spectrometry; then screened against various enzymes i.e. acetylcholinesterase,butyrylcholinesterase,lipoxygenase and α-glucosidase enzymes and five different bacterial strains. the synthesized compounds were found to be good inhibitors of lipoxygenase but moderate inhibitors of ache,bche and a-glucosidase; whereas compounds 3,5a,5f,5n and 5r were found good antibacterial compounds. the interaction between inhibitors and target enzymes (cholinestrases and lipoxygenase) was computationally observed which correlated with the experimental results.
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کلیدواژه
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Antibacterial activity; Enzyme inhibition; Ethylated sulfonamides; Lipoxygenase and molecular docking
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آدرس
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division of science and technology,university of education,township campus,lahore, Pakistan, department of chemistry,government college university,lahore, Pakistan, department of chemistry,government college university,lahore, Pakistan, department of chemistry,government college university,lahore, Pakistan, hej research institute of chemistry,international center for chemical and biological sciences,university of karachi,karachi, Pakistan, department of chemistry,islamia university of bahawalpur,bahawalpur, Pakistan, department of chemistry,islamia university of bahawalpur,bahawalpur, Pakistan, department of pharmacy,islamia university of bahawalpur,bahawalpur, Pakistan, department of pharmacy,islamia university of bahawalpur,bahawalpur, Pakistan, department of biochemistry,abdul wali khan university mardan, Pakistan, department of biochemistry,abdul wali khan university mardan, Pakistan
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Authors
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