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The discovery and structure-activity relationships of pyrano[3,4-b]indole-based inhibitors of hepatitis C virus NS5B polymerase
Authors:Jackson Randy W  LaPorte Matthew G  Herbertz Torsten  Draper Tandy L  Gaboury Janet A  Rippin Susan R  Patel Ravi  Chunduru Srinivas K  Benetatos Christopher A  Young Dorothy C  Burns Christopher J  Condon Stephen M
Institution:a VenatoRx Pharmaceuticals Inc., 700 Pennsylvania Drive, Exton, PA 19341, USA
b University of Pittsburgh, Center for Chemical Methodologies and Library Development, Pittsburgh, PA 15260, USA
c TetraLogic Pharmaceuticals, 343 Phoenixville Pike, Malvern, PA 19355, USA
d Department of Medicinal Chemistry, ViroPharma Incorporated, 730 Stockton Drive, Exton, PA 19341, USA
e Department of Computational Chemistry, ViroPharma Incorporated, 730 Stockton Drive, Exton, PA 19341, USA
f Department of Biology, ViroPharma Incorporated, 730 Stockton Drive, Exton, PA 19341, USA
Abstract:We describe the structure-activity relationship of the C7-position of pyrano3,4-b]indole-based inhibitors of HCV NS5B polymerase. Further exploration of the allosteric binding site led to the discovery of the significantly more potent compounds 13 and 14.
Keywords:HCV NS5B polymerase  Pyranoindoles
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