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. 2005 Oct 1;15(19):4180-4.
doi: 10.1016/j.bmcl.2005.06.091.

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency

A Arasappan  1 , F G Njoroge, T-Y Chan, F Bennett, S L Bogen, K Chen, H Gu, L Hong, E Jao, Y-T Liu, R G Lovey, T Parekh, R E Pike, P Pinto, B Santhanam, S Venkatraman, H Vaccaro, H Wang, X Yang, Z Zhu, B Mckittrick, A K Saksena, V Girijavallabhan, J Pichardo, N Butkiewicz, R Ingram, B Malcolm, A Prongay, N Yao, B Marten, V Madison, S Kemp, O Levy, M Lim-Wilby, S Tamura, A K Ganguly
Affiliations

Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency

A Arasappan et al. Bioorg Med Chem Lett. .

Abstract

We have discovered that introduction of appropriate amino acid derivatives at P'2 position improved the binding potency of P3-capped alpha-ketoamide inhibitors of HCV NS3 serine protease. X-ray crystal structure of one of the inhibitors (43) bound to the protease revealed the importance of the P'2 moiety.

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