Synthesis, characterization and biological screening of 5-substituted-1,3,4-oxadiazole-2yl-N-(2-methoxy-5-chlorophenyl)-2-sulfanyl acetamide

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-oxadiazo...

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Veröffentlicht in:Pakistan journal of pharmaceutical sciences 2013-03, Vol.26 (2), p.345-352
Hauptverfasser: Rehman, Azizur, Fatima, Ambreen, Abbas, Nadia, Abbasi, Muhammad Athar, Khan, Khalid Mohammed, Ashraf, Muhammad, Ahmad, Irshad, Ejaz, Syeda Abida
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Sprache:eng
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Zusammenfassung: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 (1)H-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.
ISSN:1011-601X