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...

תיאור מלא

שמור ב:
מידע ביבליוגרפי
מחבר ראשי: Hammami Maya
מחברים אחרים: Steinmetzer, Torsten (Prof. Dr.) (BetreuerIn (Doktorarbeit))
פורמט: Dissertation
שפה:אנגלית
יצא לאור: Philipps-Universität Marburg 2012
נושאים:
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תיאור
סיכום: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
DOI:10.17192/z2012.0955