Author/Editor     Obreza, A; Stegnar, M; Trampuž-Bakija, A; Preželj, A; Urleb, U
Title     Synthesis and in vitro evaluation of new azaphenylalanine derivatives as serine protease inhibitors
Type     članek
Source     Pharmazie
Vol. and No.     Letnik 59
Publication year     2004
Volume     str. 739-43
Language     eng
Abstract     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.
Descriptors     DRUG APPROVAL
TECHNOLOGY, PHARMACEUTICAL
DRUG INDUSTRY
SERINE PROTEINASE INHIBITORS
AZA COMPOUNDS
PHENYLALANINE
THROMBIN
BINDING SITES
FACTOR XA