کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1365362 | 981560 | 2008 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design and synthesis of novel potent and selective integrin αvβ3 antagonists—Novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates Design and synthesis of novel potent and selective integrin αvβ3 antagonists—Novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates](/preview/png/1365362.png)
An unexpected ring contraction of benzazepinone based αvβ3 antagonists led to the design of quinolinone-type derivatives. Novel and efficient synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates were established. Nanomolar αvβ3 antagonists based on these new scaffolds were prepared. Moreover, benzoxazinones 15a and 15b exhibited high microsomal stability and good permeability.
An unexpected ring contraction of benzazepinone based αvβ3 antagonists led to the design of quinolinone-type derivatives (X = CH2, O, NH). Novel and efficient synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates were established. Nanomolar αvβ3 antagonists based on these new scaffolds were prepared. Moreover, benzoxazinones (X = O) 15a and 15b exhibited high microsomal stability and good permeability.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 2, 15 January 2008, Pages 527–531