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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
biochemistry, genetics and molecular biology
Synthesis and evaluation of coumarin derivatives as potential dual-action HIV-1 protease and reverse transcriptase inhibitors
Bioorganic and Medicinal Chemistry, Volume 21, No. 7, Year 2013
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Description
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. © 2013 Elsevier Ltd. All rights reserved.
Authors & Co-Authors
Olomola, Temitope O.
South Africa, Grahamstown
Rhodes University
Klein, Rosalyn
South Africa, Grahamstown
Rhodes University
Mautsa, Nicodemus
South Africa, Grahamstown
Rhodes University
Sayed, Yasien
South Africa, Johannesburg
University of the Witwatersrand
Kaye, Perry T.
South Africa, Grahamstown
Rhodes University
Statistics
Citations: 79
Authors: 5
Affiliations: 2
Identifiers
Doi:
10.1016/j.bmc.2013.01.025
ISSN:
09680896
e-ISSN:
14643391
Research Areas
Infectious Diseases
Sexual And Reproductive Health
Study Approach
Qualitative