| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5269710 | Tetrahedron Letters | 2010 | 4 Pages |
Abstract
3-(Chloromethyl)coumarins, obtained via acid-catalysed cyclisation of salicylaldehyde-derived Baylis-Hillman adducts, have been treated with propargylamine; reaction of the resulting 3-alkynylmethylcoumarins with azidothymidine (AZT) in the presence of a Cu(I) catalyst has afforded a series of cycloaddition products for evaluation, in their own right, as potential dual-action HIV-1 protease and non-nucleoside reverse transcriptase inhibitors, and as scaffolds for further structural elaboration.
Graphical abstractBaylis-Hillman-derived 3-(chloromethyl)coumarins have been elaborated to afford coumarin-AZT conjugates as scaffolds for the development of potential dual-action HIV-1 PR/RT inhibitors.Download full-size image
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Authors
Temitope O. Olomola, Rosalyn Klein, Kevin A. Lobb, Yasien Sayed, Perry T. Kaye,