Citation:
XU Chang, AN Yue, ZHU Haotian, LIN Yue, WANG Rinan. Synthesis,Crystal Structure and Biological Activities of 3-Substituted-1-(5-aryl-1,3,4-thiadiazol-2-yl)-1H-pyrazole-4-formaldehyde[J]. Chinese Journal of Applied Chemistry,
;2015, 32(7): 748-758.
doi:
10.11944/j.issn.1000-0518.2015.07.140421
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Sixteen title compounds 1,3,4-thiadiazole derivatives 5a~5p and sixteen intermediates 4a~4p were synthesized using 2-amino-5-substituted-1,3,4-thiadiazoles as the starting materials.All of thirty-two compounds are new compounds.The single crystal of compound 5a was obtained by solution crystallization method.X-ray single crystal diffraction analyses show that the crystal is a triclinic crystal system,P-1 space group.The structures of the title compounds and intermediates were characterized by IR,1H NMR and elemental analyses.The antibacterial activity of compound 5 was evaluated with microdilution method.Compound 5h exhibits higher antibacterial activity to Staphylococcus aureus than the others,of which bacteriostasis rate is up to 65.30%.
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Keywords:
- thiadiazole,
- pyrazole,
- synthesis,
- structure,
- biological activity
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