188127-06-2Relevant academic research and scientific papers
Design and synthesis of conformationally constrained arginal thrombin inhibitors
Salimbeni, Aldo,Paleari, Fabio,Canevotti, Renato,Criscuoli, Marco,Lippi, Annalisa,Angiolini, Mauro,Belvisi, Laura,Scolastico, Carlo,Colombo, Lino
, p. 2205 - 2210 (2007/10/03)
A series of conformationally constrained arginal thrombin inhibitors was prepared starting from 5,6 or 5,7 bicyclic lactamic structures, that an indirect approach of X-ray structure-based drug design indicated as D-Phe-Pro dipeptide mimetics. The tetrahydrocquinolyl sulfonamido derivative Ig (LR-D/009) displayed the best inhibitory potency (IC50 = 0.018 μm), with good selectivity over plasmin and trypsin.
