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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Chi tiết về thư mục
Tác giả chính: Hammami Maya
Tác giả khác: Steinmetzer, Torsten (Prof. Dr.) (Cố vấn luận án)
Định dạng: Dissertation
Ngôn ngữ:Tiếng Anh
Được phát hành: Philipps-Universität Marburg 2012
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Tóm tắt: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