Avtor/Urednik		Obreza, A; Stegnar, M; Urleb, U
Naslov		Novel non-covalent azaphenylalanine thrombin inhibitors with an aminomethyl or amino group at the P1 position
Tip		članek
Vir		Pharmazie
Vol. in št.		Letnik 59, št. 9
Leto izdaje		2004
Obseg		str. 659-67
Jezik		eng
Abstrakt		Design, synthesis and biological evaluation of a series of novel non-covalent azaphenylalanine thrombin inhibitors are presented. Replacement of the basic benzamidine moiety in azaphenylalanine derivatives by benzylamine (P1 part of a molecule) and the introduction of a N-cyclopentyl-N-methylamine moiety in the P2 part of a molecule resulted in the thrombin inhibitor LK-733 with greatly increased selectivity against trypsin and an in vitro Ki of 31 nM.
Deskriptorji		THROMBIN DRUG INDUSTRY TECHNOLOGY, PHARMACEUTICAL DRUG APPROVAL AZA COMPOUNDS PHENYLALANINE BINDING SITES TRYPSIN SERINE PROTEINASE INHIBITORS FACTOR XA