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Resumen de Synthesis, structural characterization and enzyme inhibition studies on 5-(2-nitrostyryl)-1,3,4-oxadiazole-2-thiol derivatives

Muhammad Athar Abbasi, Adnan Akhtar, Aziz ur-rehman, Khadija Nafeesa, Sabahat Zahra Siddiqui, Khalid Mohammed Khan, Muhammad Ashraf, Syeda Abida Ejaz

  • In the present work, S-substituted derivatives of 5-(2-nitrostyryl)-1,3,4-oxadiazole-2-thiol (4) were synthesized by successive conversions of 3-(2-nitrophenyl) acrylic acid (1) into its respective ester, hydrazide and 1,3,4-oxadiazole. Finally the target compounds were obtained by reaction of 5-(2-nitrostyryl)-1,3,4-oxadiazole-2-thiol (4) with a series of various electrophiles, (5a-I), in NN-dimethyl formamide (DMF) in the presence of sodium hydride (NaH). The structural characterization of these newly synthesized compounds was done by IR, ¹H-NMR, HR-MS and EI-MS spectral data. All these compounds were evaluated for their enzyme inhibitory potentials and found to exhibit broad range spectrum against acetylcholinesterase, butyrylcholinestrase and lipoxygenase enzymes.


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