Avtor/Urednik		Zega, Anamarija; Mlinšek, Gregor; Šolmajer, Tomaž; Trampuš-Bakija, Alenka; Stegnar, Mojca; Urleb, Uroš
Naslov		Thrombin inhibitors built on an azaphenymalaline scaffold
Tip		članek
Vir		Bioorg Med Chem Lett
Vol. in št.		Letnik 14
Leto izdaje		2004
Obseg		str. 1563-7
Jezik		eng
Abstrakt		A series of azaphenylalanine derivatives were investigated as novel thrombin inhibitors based on the prodrug principle. By systematic structural modifications we have identified optimal groups for this series that led us to potent inhibitors of thrombin incorporating the benzamidine fragment at the P1 position, and their potentially orally active benzamidoxime prodrugs. The binding modes in the thrombin active site of two representative compounds were identified by X-ray crystallographic analysis.
Deskriptorji		THROMBIN AZA COMPOUNDS PHENYLALANINE BENZAMIDINES BINDING SITES CRYSTALLOGRAPHY, X-RAY DRUG INDUSTRY