372982-89-3Relevant academic research and scientific papers
Thrombin inhibitors
-
Page/Page column 29, (2010/01/31)
The invention relates to compounds of formula I D—CO—B—A-Het and pharmaceutically acceptable salts thereof where substituents in description have the specified meanings. The compounds are used as thrombin inhibitors.
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P1-arginine mimetics
Peterlin-Masic, Lucija,Mlinsek, Gregor,Solmajer, Tomaz,Trampus-Bakija, Alenka,Stegnar, Mojca,Kikelj, Danijel
, p. 789 - 794 (2007/10/03)
The design, synthesis and biological activity of non-covalent thrombin inhibitors incorporating 4,5,6,7-tetrahydroindazole, 2-methyl-4,5,6,7-tetrahydroindazole, 4,5,6,7-tetrahydroisoindole, 5,6,7,8-tetrahydroquinazoline and 5,6,7,8-tetrahydroquinazolin-2-amine as novel, partially saturated, heterobicyclic P1-arginine side-chain mimetics is described. The binding mode of the most potent candidate in the series co-crystallized with human α-thrombin, which exhibited an in vitro Ki of 140 nM and more that 478-fold selectivity against trypsin, is discussed.
