Author/Editor | Kranjc, Andreja; Peterlin-Mašič, Lucija; Ilaš, Janez; Preželj, Andrej; Stegnar, Mojca; Kikelj, Danijel | |
Title | Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties | |
Type | članek | |
Source | Bioorg Med Chem Lett | |
Vol. and No. | Letnik 14, št. 12 | |
Publication year | 2004 | |
Volume | str. 3251-6 | |
Language | eng | |
Abstract | Optimization of lead compounds 1 and 2 resulted in novel, selective, and potent thrombin inhibitors incorporating weakly basic heterobicyclic Pl-arginine mimetics. The design, synthesis, and biological activity of racemic thrombin inhibitors 17-29 and enantiomerically pure thrombin inhibitors 30-33 are described. The arginine side-chain mimetics used in this study are 4,5,6,7tetrahydro-l,3-benzothiazol-2-amine, 4,5,6,7-tetrahydro-2H-indazole, and 2-imino-4,5,6,7-tetrahydro-l,3-benzothiazol-3(2H)-ylamine. | |
Descriptors | THROMBIN ANTICOAGULANTS PYRIDONES ACETAMIDES ARGININE STEREOISOMERISM THROMBIN TIME PROTHROMBIN TIME PARTIAL THROMBOPLASTIN TIME TRYPSIN |