期刊
BIOORGANIC CHEMISTRY
卷 80, 期 -, 页码 189-194出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2018.06.005
关键词
Coumarinopyrazole; 1,2,3-triazole; Click chemistry; Anticholinesterase; Anti-5-lipoxygenase; Anti-tyrosinase; Cytotoxic; SAR
A series of new 1,2,3-triazole linked coumarinopyrazole conjugates 4a-e and 5a-e have been synthesized via the Copper(I)-catalysed Alkyne-Azide Cycloaddition (CuAAC). Going through the reaction of compound 2 with the 3-propargyl bromide gave a mixture of propargylated regioisomers 3 + 3' used as a dipolarophile to access to triazoles 4a-e and 5a e. The structures of the prepared cycloadducts were determined by H-1, C-13 and 2D-NMR techniques and by HAMS analysis. All the synthesized derivatives have been evaluated for their anticholinesterase, anti-5-lipoxygenase, anti-tyrosinase, and cytotoxic activities.
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