Novel Non-nucleoside Inhibitors of HIV-1 Reverse Transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones

We have explored the potential of derivatives of the dipyrido[2,3-b:2',3'-e][1,4]diazepinone ring system as inhibitors of HIV-1 reverse transcriptase (RT). These compounds are isomeric to the potent RT inhibitor nevirapine and are available via a novel Smiles rearrangement on intermediates...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 38; no. 8; pp. 1406 - 1410
Main Authors Proudfoot, John R, Patel, Usha R, Kapadia, Suresh R, Hargrave, Karl D
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.04.1995
Subjects
AIDS/HIV
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Azepines - chemistry
Azepines - pharmacology
HIV Reverse Transcriptase
HIV-1 - drug effects
HIV-1 - enzymology
human immunodeficiency virus 1
Magnetic Resonance Spectroscopy
Reverse Transcriptase Inhibitors
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Summary:We have explored the potential of derivatives of the dipyrido[2,3-b:2',3'-e][1,4]diazepinone ring system as inhibitors of HIV-1 reverse transcriptase (RT). These compounds are isomeric to the potent RT inhibitor nevirapine and are available via a novel Smiles rearrangement on intermediates used for the synthesis of nevirapine analogs. Derivatives of this isomeric series are weaker inhibitors of RT than corresponding nevirapine analogs, although with appropriate substitution of the A- and C-pyridine rings activity can be improved.
Bibliography:istex:2132C9662430ED2BE8EBEDB85254CE2047D44EC5
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ISSN:0022-2623
1520-4804
DOI:10.1021/jm00008a019