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Development of new inhibitors for the type II transmembrane serine protease matriptase
Several new inhibitors were prepared and tested as potential matriptase inhibitors. The most potent compounds were found among the tertiary amides of arylsulfonylated-3-amidinophenylalanines. The incorporation of suitable bis-substituted biphenylsulfonyl groups in combination with appropriate C-term...
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| Format: | Dissertation |
| Langue: | anglais |
| Publié: |
Philipps-Universität Marburg
2012
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| Accès en ligne: | Texte intégral en PDF |
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| Résumé: | Several new inhibitors were prepared and tested as potential matriptase inhibitors. The most potent compounds were found among the tertiary amides of arylsulfonylated-3-amidinophenylalanines. The incorporation of suitable bis-substituted biphenylsulfonyl groups in combination with appropriate C-terminal urea structures provided the final strong potent monobasic matriptase inhibitors with acceptable selectivity against related trypsin-like serine proteases. Such compounds are suitable candidates for their further evaluation in cell culture experiments to elucidate the potential role of matriptase in pathophysiological processes |
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| DOI: | 10.17192/z2012.0955 |