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P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease
E Scott Priestley1, Indawati De Lucca, Bahman Ghavimi
1Bristol-Myers Squibb Pharmaceutical Research Institute, Experimental Station, Wilmington,DE 19880-0500, USA. scott.priestley@bms.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
Abstract:
A series of peptide boronic acids containing extended, hydrophobic P1 residues was prepared to probe the shallow, hydrophobic S1 region of HCV NS3 protease. The p-trifluoromethylphenethyl P1 substituent was identified as optimal with respect to inhibitor potency for NS3 and selectivity against elastase and chymotrypsin.