100868-47-1Relevant articles and documents
2-pyridinone derivatives: A new class of nonucleoside, HIV-1-specific reverse transcriptase inhibitors [3]
Saari,Hoffman,Wai,Fisher,Rooney,Smith,Thomas,Goldman,O'Brien,Nunberg,Quintero,Schleif,Emini,Stern,Anderson
, p. 2922 - 2925 (1991)
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Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one
Saari, Walfred S.,Wai, John S.,Fisher, Thorsten E.,Thomas, Craig M.,Hoffman, Jacob M.,et al.
, p. 3792 - 3802 (2007/10/02)
A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
The metabolism of 2:4-,2:5-and 3:4-dichloronitrobenzene in the rabbit.
BRAY,JAMES,THORPE
, p. 483 - 490 (2007/10/14)
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