A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate a...A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate as a catalyst.Confirmation of the synthetic structure of the titled compounds(4-16)was substantiated by thin-layer chromatography(TLC),IR,^(1)H NMR,^(13)C NMR,Mass spectra(MS)and elemental analysis(C,H,and N)were finished.The titled compounds were assessed for anticholinesterase activity against acetylcholinesterase and butyl cholinesterase enzymes.The titled compound produced weak,moderate,or high anticholinesterase activity.Particularly,compound 8 demonstrated the best anticholinesterase activity of all the 1,4-dihydropyridines,with an IC_(50) estimation of 0.08μM and 2.9μM.展开更多
文摘A novel Acetazolamide condensed 1,4-dihydropyridines was set up by treating of N-(5-acetamido-1,3,4-thiadiazol-2-ylsulfonyl)-3-oxobutanamide with an aryl aldehyde and 25-30%alkali with sight amount of barium nitrate as a catalyst.Confirmation of the synthetic structure of the titled compounds(4-16)was substantiated by thin-layer chromatography(TLC),IR,^(1)H NMR,^(13)C NMR,Mass spectra(MS)and elemental analysis(C,H,and N)were finished.The titled compounds were assessed for anticholinesterase activity against acetylcholinesterase and butyl cholinesterase enzymes.The titled compound produced weak,moderate,or high anticholinesterase activity.Particularly,compound 8 demonstrated the best anticholinesterase activity of all the 1,4-dihydropyridines,with an IC_(50) estimation of 0.08μM and 2.9μM.
