Structure-activity relationship of new anti-hepatitis C virus agents: Heterobicycle-coumarin conjugates

Johan Neyts, Erik De Clercq, Raghunath Singha, Yung Hsiung Chang, Asish R. Das, Subhasish K. Chakraborty, Shih Ching Hong, Shwu Chen Tsay, Ming Hua Hsu, Jih Ru Hwu

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Abstract

For establishment of the structure-activity relationship, 19 heterobicycle-coumarin conjugated compounds with the -SCH2- linker were synthesized and found to possess significant antiviral activities. Prominent examples included imidazopyridine-coumarin 12c, purine-coumarin 12d, and benzoxazole-coumarin 14c, which inhibited HCV replication at an EC 50 of 6.8, 2.0, and 12 μM, respectively. The heteroatoms in bicycles and the substituent effect on coumarin played essential roles.

Original languageEnglish
Pages (from-to)1486-1490
Number of pages5
JournalJournal of Medicinal Chemistry
Volume52
Issue number5
DOIs
Publication statusPublished - 2009 Mar 12

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

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    Neyts, J., De Clercq, E., Singha, R., Chang, Y. H., Das, A. R., Chakraborty, S. K., Hong, S. C., Tsay, S. C., Hsu, M. H., & Hwu, J. R. (2009). Structure-activity relationship of new anti-hepatitis C virus agents: Heterobicycle-coumarin conjugates. Journal of Medicinal Chemistry, 52(5), 1486-1490. https://doi.org/10.1021/jm801240d