Author/Editor		Peterlin-Mašič, Lucija; Mlinšek, Gregor; Šolmajer, Tomaž; Trampuš-Bakija, Alenka; Stegnar, Mojca; Kikelj, Danijel
Title		Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics
Type		članek
Source		Bioorg Med Chem Lett
Vol. and No.		Letnik 13
Publication year		2003
Volume		str. 789-94
Language		eng
Abstract		The design, synthesis and biological activity of non-covalent thrombin inhibitors incorporating 4,5,6,7-tetrahydroindazole, 2-methyl-4,5,6,7-tetrahydroindawle, 4,5,6,7-tetrahydroisoindole, 5,6,7,8-tetrahydroquinazoline and 5,6,7,8-tetrahydroquinazolin-2-amine as novel, partially saturated, heterobicyclic P'-arginine side-chain mimetics is described. The binding mode of the most potent candidate in the series co-crystallized with human x-thrombin, which exhibited an in vitro K1 of 140 nM and more that 478-fold selectivity against trypsin, is discussed.
Descriptors		THROMBIN INDAZOLES QUINAZOLINES INDOLES ARGININE