Development and characterization of new peptidomimetic inhibitors of the West Nile virus NS2B-NS3 protease

Potent inhibitors of the West Nile virus NS2B-NS3 protease could be useful drugs for the treatment of WNV infections. Therefore, in the present work, new substrate analogue inhibitors against the WNV protease have been developed. In this present work, new decarboxylated arginine memtics inhibitors...

Ausführliche Beschreibung

Gespeichert in:
1. Verfasser: Hammamy, M. Zouhir
Beteiligte: Steinmetzer, Torsten (Prof. Dr.) (BetreuerIn (Doktorarbeit))
Format: Dissertation
Sprache:Englisch
Veröffentlicht: Philipps-Universität Marburg 2014
Pharmazeutische Chemie
Ausgabe:http://dx.doi.org/10.17192/z2014.0245
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Zusammenfassung:Potent inhibitors of the West Nile virus NS2B-NS3 protease could be useful drugs for the treatment of WNV infections. Therefore, in the present work, new substrate analogue inhibitors against the WNV protease have been developed. In this present work, new decarboxylated arginine memtics inhibitors against the WNV NS2B-NS3 protease were developed. In comparison to the known agmatine derivatives, the P1 trans-4-Guanidinocyclohexylmethylamid containing inhibitors have higher potency and selectivity against the WNV. Moreover, the first crystal structure of the WNV protease in complex with small noncovalently-binding inhibitor was solved.
DOI:http://dx.doi.org/10.17192/z2014.0245