Title of article :
Synthesis, characterization and biological screening of 5-substituted-1,3,4-oxadiazole-2yl-N-(2-methoxy-5-chlorophenyl)-2-sulfanyl acetamide
Author/Authors :
ur-Rehman, Aziz Government College University - Department of Chemistry, Pakistan , Fatima, Ambreen Government College University - Department of Chemistry, Pakistan , Abbas, Nadia Government College University - Department of Chemistry, Pakistan , Abbasi, Muhammad Athar Government College University - Department of Chemistry, Pakistan , Khan, Khalid Mohammed University of Karachi - HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, Pakistan , Ashraf, Muhammad Islamia University of Bahawalpur - Department of Biochemistry and Biotechnology, Pakistan , Ahmad, Irshad Islamia University of Bahawalpur - Department of Biochemistry and Biotechnology, Pakistan , Ejaz, Syeda Abida Islamia University of Bahawalpur - Department of Pharmacy, Pakistan
Abstract :
In the current study, a series of 5-substituted-1,3,4-oxadiazole-2yl-N-(2-methoxy-5-chlorophenyl)-2-sulfanyl acetamide was synthesized by converting variously substituted/unsubstituted aromatic organic acids successively into the corresponding esters, hydrazides and then 5-substituted-1,3,4-oxadiazole-2-thiols. Finally the target compounds were obtained by stirring 5-substituted-1,3,4-oxadiazole-2-thiols with N-(2-methoxy-5-chlorophenyl)-2-bromoacetamide in the presence of N,N-dimethyl formamide (DMF) and sodium hydride (NaH). The structures of the synthesized compounds were confirmed based on 1H-NMR, IR and mass spectral data. The synthesized compounds were screened against acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and lipoxygenase enzymes (LOX) and were found to be relatively more active against acetyl cholinesterase.
Keywords :
Aromatic acids , oxadiazoles , acetylcholinesterase , 1H , NMR and EI , MS
Journal title :
Pakistan Journal Of Pharmaceutical Sciences
Journal title :
Pakistan Journal Of Pharmaceutical Sciences
