Capped dipeptide alpha-ketoacid inhibitors of the HCV NS3 protease |
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Authors: | Nizi Emanuela Koch Uwe Ponzi Simona Matassa Victor G Gardelli Cristina |
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Institution: | Department of Chemistry, IRBM, MRL Rome, Via Pontina Km 30,600, Pomezia, 00040 Rome, Italy. |
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Abstract: | The N-terminal aminoacid of alpha-ketotripeptide inhibitors of the hepatitis C virus NS3 protease can be replaced with an alpha-hydroxy acid, leading to capped dipeptide inhibitors such as 20 with an IC(50) value of 3.0 microM. The importance of the lipophilic side chain interactions at S3 of the protease and the requirement of the capping residue with R configuration have been explained by molecular modeling studies. |
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