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Baylis-Hillman-derived 3-(benzylaminomethyl)coumarins have been treated, sequentially, with chloroacetyl chloride and propargylamine to afford alkynylated coumarins as substrates for Click Chemistry reactions with azidothymidine (AZT) in the presence of a Cu(I) catalyst. The dual-action HIV-1 protease (PR) and reverse transcriptase (RT) inhibition potential of the resulting N-benzylated cycloaddition products, and a series of non-benzylated analogues, has been explored using saturation transfer difference (STD) NMR, computer modelling and enzyme inhibition techniques. Copyright © 2013 Elsevier Ltd. All rights reserved.


Temitope O Olomola, Rosalyn Klein, Nicodemus Mautsa, Yasien Sayed, Perry T Kaye. Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors. Bioorganic & medicinal chemistry. 2013 Apr 1;21(7):1964-71

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PMID: 23415084

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