Bioorganic and Medicinal Chemistry Letters p. 2205 - 2210 (1997)
Update date:2022-08-04
Topics:
Salimbeni, Aldo
Paleari, Fabio
Canevotti, Renato
Criscuoli, Marco
Lippi, Annalisa
Angiolini, Mauro
Belvisi, Laura
Scolastico, Carlo
Colombo, Lino
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.
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