کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376395 | 981957 | 2008 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase Discovery of triazolinone non-nucleoside inhibitors of HIV reverse transcriptase](/preview/png/1376395.png)
Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against several NNRTI-resistant virus strains. Pharmacokinetic studies indicated that inhibitor 7e has good bioavailability in rats. Several fragments of inhibitor 7c were prepared, and the binding of these compounds to HIV-RT was analyzed by surface plasmon resonance spectroscopy.
Novel diaryl ether HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) were prepared. Triazolinone compounds that strongly inhibit wild-type and NNRTI-resistant viruses and display excellent pharmacokinetic properties were identified.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 15, 1 August 2008, Pages 4348–4351