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Structure−Activity Relationship of New Anti-Hepatitis C Virus Agents: Heterobicycle−Coumarin Conjugates

2009; American Chemical Society; Volume: 52; Issue: 5 Linguagem: Inglês

10.1021/jm801240d

1520-4804

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

Quinazolinone synthesis and applications

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 EC50 of 6.8, 2.0, and 12 μM, respectively. The heteroatoms in bicycles and the substituent effect on coumarin played essential roles.