Article
Discovery of tricyclic 5,6-dihydro-1H-pyridin-2-ones as novel, potent, and orally bioavailable inhibitors of HCV NS5B polymerase.
Bioorganic & medicinal chemistry letters - 15 Nov 2009
Ruebsam Frank, Murphy Douglas E, Tran Chinh V, Li Lian-Sheng, Zhao Jingjing, Dragovich Peter S, McGuire Helen M, Xiang Alan X, Sun Zhongxiang, Ayida Benjamin K, Blazel Julie K, Kim Sun Hee, Zhou Yuefen, Han Qing, Kissinger Charles R, Webber Stephen E, Showalter Richard E, Shah Amit M, Tsan Mei, Patel Rupal A, Thompson Peggy A, Lebrun Laurie A, Hou Huiying J, Kamran Ruhi, Sergeeva Maria V, Bartkowski Darian M, Nolan Thomas G, Norris Daniel A, Khandurina Julia, Brooks Jennifer, Okamoto Ellen, Kirkovsky Leo
Abstract excerpt
A novel series of non-nucleoside small molecules containing a tricyclic dihydropyridinone structural motif was identified as potent HCV NS5B polymerase inhibitors. Driven by structure-based design and building on our previous efforts in related series of molecules, we undertook extensive SAR studies, in which we identified a number of metabolically stable and very potent compounds in genotype 1a and 1b replicon...
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.