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

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

Pakistan journal of pharmaceutical sciences (2013-03-05)
Azizur Rehman, Ambreen Fatima, Nadia Abbas, Muhammad Athar Abbasi, Khalid Mohammed Khan, Muhammad Ashraf, Irshad Ahmad, Syeda Abida Ejaz
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.

MATERIALIEN
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Marke
Produktbeschreibung

Sigma-Aldrich
Acetylcholinesterase aus Electrophorus electricus (electric eel), Type VI-S, lyophilized powder, 200-1,000 units/mg protein
Sigma-Aldrich
Lipoxidase Zubereitung aus Glycine max (soybean), Type I-B, lyophilized powder, ≥50,000 units/mg solid
Sigma-Aldrich
Acetylcholinesterase aus Electrophorus electricus (electric eel), Type V-S, lyophilized powder, ≥1,000 units/mg protein
Sigma-Aldrich
Acetylcholinesterase human, recombinant, expressed in HEK 293 cells, lyophilized powder, ≥1,000 units/mg protein (BCA)
Sigma-Aldrich
Acetylcholinesterase aus Humanerythrocyten, buffered aqueous solution, ≥500 units/mg protein (BCA)
Sigma-Aldrich
Lipoxidase Zubereitung aus Glycine max (soybean), Type V, ammonium sulfate suspension, 500,000-1,000,000 units/mg protein