|
Title
|
|
|
|
Synthesis and biological evaluation of C-5 methyl substituted 4-arylthio and 4-aryloxy-3-iodopyridin-2(1H)-one type anti-HIV agents
|
|
|
Author
|
|
|
|
|
|
|
Abstract
|
|
|
|
| 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. |
|
|
|
Language
|
|
|
|
English
|
|
|
Source (journal)
|
|
|
|
Journal of medicinal chemistry. - Washington, D.C., 1963, currens
|
|
|
Publication
|
|
|
|
Washington, D.C.
:
2009
|
|
|
ISSN
|
|
|
|
0022-2623
[print]
1520-4804
[online]
|
|
|
Volume/pages
|
|
|
|
52
:23
(2009)
, p. 7473-7487
|
|
|
ISI
|
|
|
|
000272338000017
|
|
|
Full text (Publisher's DOI)
|
|
|
|
|
|