Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates

An unexpected ring contraction of benzazepinone based alpha(nu)beta(3) antagonists led to the design of quinolinone-type derivatives. Novel and efficient synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates were established. Nanomolar alpha(nu)beta(3) antagonists based on th...

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Published inBioorganic & medicinal chemistry letters Vol. 18; no. 2; pp. 527 - 531
Main Authors Seitz, Werner, Geneste, Hervé, Backfisch, Gisela, Delzer, Jürgen, Graef, Claudia, Hornberger, Wilfried, Kling, Andreas, Subkowski, Thomas, Zimmermann, Norbert
Format Journal Article
LanguageEnglish
Published England 15.01.2008
Subjects
Benzoxazines - chemical synthesis
Benzoxazines - chemistry
Benzoxazines - pharmacology
Drug Design
Enzyme-Linked Immunosorbent Assay
Integrin alphaVbeta3 - antagonists & inhibitors
Isoquinolines - chemical synthesis
Isoquinolines - chemistry
Isoquinolines - pharmacology
Quinazolines - chemical synthesis
Quinazolines - chemistry
Quinazolines - pharmacology
Structure-Activity Relationship
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Summary:An unexpected ring contraction of benzazepinone based alpha(nu)beta(3) antagonists led to the design of quinolinone-type derivatives. Novel and efficient synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates were established. Nanomolar alpha(nu)beta(3) antagonists based on these new scaffolds were prepared. Moreover, benzoxazinones 15a and 15b exhibited high microsomal stability and good permeability.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:1464-3405