丙型肝炎病毒NS3-4A丝氨酸蛋白酶抑制剂：具有更高活性的P'2部分的构效关系
Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P'2 moiety with improved potency.
作者信息
Arasappan A, Njoroge F G, Chan T-Y, Bennett F, Bogen S L, Chen K, Gu H, Hong L, Jao E, Liu Y-T, Lovey R G, Parekh T, Pike R E, Pinto P, Santhanam B, Venkatraman S, Vaccaro H, Wang H, Yang X, Zhu Z, Mckittrick B, Saksena A K, Girijavallabhan V, Pichardo J, Butkiewicz N, Ingram R, Malcolm B, Prongay A, Yao N, Marten B, Madison V, Kemp S, Levy O, Lim-Wilby M, Tamura S, Ganguly A K
机构信息
Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4180-4. doi: 10.1016/j.bmcl.2005.06.091.
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.
我们发现，在P'2位引入合适的氨基酸衍生物可提高丙型肝炎病毒NS3丝氨酸蛋白酶的P3封端α-酮酰胺抑制剂的结合效力。其中一种与该蛋白酶结合的抑制剂（43）的X射线晶体结构揭示了P'2部分的重要性。
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