Design, synthesis and biological evaluation of novel 1,2,3-triazole linked coumarinopyrazole conjugates as potent anticholinesterase, anti-5-lipoxygenase, anti-tyrosinase and anti-cancer agents.

Abstract:

: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 1H, 13C and 2D-NMR techniques and by HRMS analysis. All the synthesized derivatives have been evaluated for their anticholinesterase, anti-5-lipoxygenase, anti-tyrosinase, and cytotoxic activities.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Chekir S,Debbabi M,Regazzetti A,Dargère D,Laprévote O,Ben Jannet H,Gharbi R

doi

10.1016/j.bioorg.2018.06.005

subject

Has Abstract

pub_date

2018-10-01 00:00:00

pages

189-194

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30389-4

journal_volume

80

pub_type

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