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- W2003783193 abstract "Based on a previously identified HCV replication (replicase) inhibitor 1, SAR efforts were conducted around the pyrimidine core to improve the potency and pharmacokinetic profile of the inhibitors. A benzothiazole moiety was found to be the optimal substituent at the pyrimidine 5-position. Due to potential reactivity concern, the 4-chloro residue was replaced by a methyl group with some loss in potency and enhanced rat in vivo profile. Extensive investigations at the C-2 position resulted in identification of compound 16 that demonstrated very good replicon potency, selectivity and rodent plasma/target organ concentration. Inhibitor 16 also demonstrated good plasma levels and oral bioavailability in dogs, while monkey exposure was rather low. Chemistry optimization towards a practical route to install the benzothiazole moiety resulted in an efficient direct C-H arylation protocol." @default.
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- W2003783193 date "2012-05-01" @default.
- W2003783193 modified "2023-10-16" @default.
- W2003783193 title "5-Benzothiazole substituted pyrimidine derivatives as HCV replication (replicase) inhibitors" @default.
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- W2003783193 doi "https://doi.org/10.1016/j.bmcl.2012.03.036" @default.
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