SYNTHESIS, STRUCTURAL CHARACTERIZATION AND ENZYME INHIBITION STUDIES ON 5-(2-NITROSTYRYL)-1,3,4-OXADIAZOLE-2-THIOL DERIVATIVES

Journal of The Chilean Chemical Society

ASHRAF, MUHAMMAD¹  AKHTAR, ADNAN²  SIDDIQUI, SABAHAT ZAHRA²  AZIZ-UR-REHMAN,²  ABBASI, MUHAMMAD ATHAR²  NAFEESA, KHADIJA²  EJAZ, SYEDA ABIDA³  KHAN, KHALID MOHAMMED⁴ 

[1] Department of Biochemistry and Biotechnology, Pakistan;Government College University, Lahore, Pakistan;The Islamia University of Bahawalpur, Bahawalpur, Pakistan;University of Karachi, Karachi, Pakistan

关键词: 3-;    (2-;    nitrophenyl)acrylic acid;    5-;    (2-;    nitrostyryl)-;    1;    3;    4-;    oxadiazole-;    2-;    thiol;    1H-;    NMR;    EI-;    MS;    enzymatic activities.;   

DOI  :  10.4067/S0717-97072013000400061

学科分类：化学（综合）

来源: Sociedad Chilena de Quimica

【 摘 要 】

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.

【 授权许可】

Unknown