Author/Editor		Zega, Anamarija; Mlinšek, Gregor; Šolmajer, Tomaž; Trampuš-Bakija, Alenka; Stegnar, Mojca; Urleb, Uroš
Title		Thrombin inhibitors built on an azaphenymalaline scaffold
Type		članek
Source		Bioorg Med Chem Lett
Vol. and No.		Letnik 14
Publication year		2004
Volume		str. 1563-7
Language		eng
Abstract		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.
Descriptors		THROMBIN AZA COMPOUNDS PHENYLALANINE BENZAMIDINES BINDING SITES CRYSTALLOGRAPHY, X-RAY DRUG INDUSTRY