ANTIVIRAL COMPOUNDS

摘要

PURPOSE: New benzimidazole compounds inhibiting the growth of picornaviruses and having a desirable pharmaceutical profile are provided which are safe toxicologically. CONSTITUTION: A series of benzimidazole compounds(I) which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengovirus and flaviviruses such as hepatitis C and bovine diarrheal virus are described. In formula, a is 0, 1, 2 or 3; R is independently H, halo, cyano, amino, halo(C1-C6) alkyl, di(C1-C4) alkylamino, azido, C1-C6 alkyl, carbamoyl, piperidino, or morpholino; R0 is H, halo, C1-C4 alkyl, or C1-C4 alkoxy; R1 is halo, cyano, hydroxy, methyl, ethyl, methoxy, ethoxy, methylthio, methylsulfinyl or methylsulfonyl; R2 is H, amino or -NHC(O)(C1-C6 alkyl); R3 is dimethylamino, C1-C10 alkyl, substituted C3-C7 cycloalkyl, phenyl, thienyl, thiazoyl, piperidino, or morpholino; R4, R5 are independently H or C1-C4 alkyl are described.