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Structure-activity relationship of new anti-hepatitis C virus agents: heterobicycle-coumarin conjugates
Johan Neyts1, Erik De Clercq, Raghunath Singha
1Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium. johan.neyts@rega.kuleuven.be
Abstract:
For establishment of the structure-activity relationship, 19 heterobicycle-coumarin conjugated compounds with the -SCH(2)- 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 microM, respectively. The heteroatoms in bicycles and the substituent effect on coumarin played essential roles.
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