Improving the selectivity of 3-amidinophenylalanine-derived matriptase inhibitors

A rational structure-based approach was employed to develop novel 3-amidinophenylalanine-derived matriptase inhibitors with improved selectivity against thrombin and factor Xa. Of all 23 new derivatives, several monobasic inhibitors exhibit high matriptase affinities and strong selectivity against t...

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Veröffentlicht in:	European journal of medicinal chemistry 2022-08, Vol.238, p.114437-114437, Article 114437
Hauptverfasser:	Pilgram, Oliver, Keils, Aline, Benary, Gerrit E., Müller, Janis, Merkl, Stefan, Ngaha, Sandrine, Huber, Simon, Chevillard, Florent, Harbig, Anne, Magdolen, Viktor, Heine, Andreas, Böttcher-Friebertshäuser, Eva, Steinmetzer, Torsten
Format:	Artikel
Sprache:	eng
Schlagworte:	Antiviral potency Crystal structure determination Inhibitor design Matriptase Synthesis
Online-Zugang:	Volltext
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