Avtor/Urednik | Obreza, A; Stegnar, M; Trampuž-Bakija, A; Preželj, A; Urleb, U | |
Naslov | Synthesis and in vitro evaluation of new azaphenylalanine derivatives as serine protease inhibitors | |
Tip | članek | |
Vir | Pharmazie | |
Vol. in št. | Letnik 59 | |
Leto izdaje | 2004 | |
Obseg | str. 739-43 | |
Jezik | eng | |
Abstrakt | New inhibitors of serine proteases with azaphenylaianine scaffold were synthesized and their activity was evaluated in vitro. We studied the effect of different substituents in the part of a molecule that binds in the distal pocket of the thrombin active site. Modifications generally led to decreased activity, however two derivatives are promising lead compounds as new thrombin and dual thrombin-factor Xa inhibitors. | |
Deskriptorji | DRUG APPROVAL TECHNOLOGY, PHARMACEUTICAL DRUG INDUSTRY SERINE PROTEINASE INHIBITORS AZA COMPOUNDS PHENYLALANINE THROMBIN BINDING SITES FACTOR XA |