Author/Editor     Peterlin-Mašič, Lucija; Kranjc, Andreja; Marinko, Petra; Mlinšek, Gregor; Šolmajer, Tomaž; Stegnar, Mojca; Kikelj, Danijel
Title     Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics
Type     članek
Source     Bioorg Med Chem Lett
Vol. and No.     Letnik 13
Publication year     2003
Volume     str. 3171-7
Language     eng
Abstract     Novel, highly selective and potent thrombin inhibitors were identified as a result of combing the 3-benzylsulfonylamino2-pyridinone acetamide P2-P3 surrogate with weakly basic partially saturated heterobicyclic P1-arginine mimetics 1-8. The design, synthesis, biological activity, and the binding modes of non-covalent thrombin inhibitors featuring P1-4,5,6,7-tetrahydroindazole, 5,6,7,8-tetrahydroquinazoline, and 4,5,6,7-tetrahydrobenzothiazole moieties are described.
Descriptors     THROMBIN
PYRIDONES
ARGININE
INDAZOLES
QUINAZOLINES
HETEROCYCLIC COMPOUNDS