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Fused heterocyclic amido compounds as anti-hepatitis C virus agents. 2011
Hiroshi Aoyama, and
Kazuyuki Sugita, and
Masahiko Nakamura, and
Atsushi Aoyama, and
Mohammed T A Salim, and
Mika Okamoto, and
Masanori Baba, and
Yuichi Hashimoto
Institute of Molecular and Cellular Biosciences, The University of Tokyo, Tokyo, Japan. aoyama@iam.u-tokyo.ac.jp
We identified a fused heteroaromatic amido structure based on the phenanthridine skeleton as a superior scaffold for candidate drugs with potent anti-HCV activity. Among the compounds synthesized, a phenanthridine analogue with a 1,3-dioxolyl group (24) possessed the most potent anti-HCV activity (EC(50) value: 50 nM), with acceptable cytotoxicity. The structural development and structure-activity relationships of these compounds are described.
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