Synthesis and anticholinesterase activity of a novel series of acetazolamide condensed 1,4-dihydropyridines  

作　　者：Mudduluru Niranjan Babu Karthikeyan Elumalai Sivaneswari Srinivasan Kalpana Eluri Manogaran Elumalai Srinivasan Sivannan 

机构地区：[1]Department of Phytochemistry,Seven Hills College of Pharmacy,Tirupati 517561,India [2]Department of Medicinal Chemistry,Seven Hills College of Pharmacy,Tirupati 517561,India [3]Department of Pharmaceutics,K.K.College of Pharmacy,Chennai 600122,India [4]Faculty of Pharmaceutical Sciences,UCSI University,Cheras,Kuala Lumpur 56000,Malaysia [5]Department of Pharmacy Practice,Togari Veeramallappa Memorial College of Pharmacy,Ballari,India

出　　处：《Carbon Resources Conversion》2019年第3期191-197,共7页碳资源转化（英文）

摘　　要：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.

关 键 词：ACETAZOLAMIDE ANTICHOLINESTERASE 1 4-Dihydropyridines ACETYLCHOLINESTERASE Butyl cholinesterase 

分 类 号：O62[理学—有机化学]