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Title
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Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-iodopyridin-2(1H)-one type anti-HIV agents
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Author
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Abstract
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| A series of C-5 methyl substituted 4-arylthio- and 4-aryloxy-3-iodopyridin-2(1H)-ones has been synthesized as new pyridinone analogues for their evaluation as anti-HIV inhibitors. The optimization at the 5-position was developed through an efficient use of the key intermediates 5-ethoxycarbonyl- and 5-cyano-pyridin-2(1H)-ones (14 and 15). Biological studies revealed that several compounds show potent HIV-1 reverse transcriptase inhibitory properties, for example, compounds 93 and 99 are active at 0.6−50 nM against wild type HIV-1 and a panel of major simple/double HIV mutant strains. |
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Language
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English
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Source (journal)
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Journal of medicinal chemistry. - Washington, D.C., 1963, currens
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Publication
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Washington, D.C.
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2009
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ISSN
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0022-2623
[print]
1520-4804
[online]
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DOI
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10.1021/JM900802Y
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Volume/pages
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52
:23
(2009)
, p. 7473-7487
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ISI
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000272338000017
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Full text (Publisher's DOI)
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