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- W2091873855 abstract "A series of pyrimidine benzamide-based thrombopoietin receptor agonists is described. The lead molecule contains a 2-amino-5-unsubstituted thiazole, a group that has been associated with idiosyncratic toxicity. The potential for metabolic oxidation at C-5 of the thiazole, the likely source of toxic metabolites, was removed by substitution at C-5 or by replacing the thiazole with a thiadiazole. Potency in the series was improved by modifying the substituents on the pyrimidine and/or on the thiazole or thiadiazole pendant aryl ring. In vivo examination revealed that compounds from the series are not highly bioavailable. This is attributed to low solubility and poor permeability." @default.
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- W2091873855 date "2007-10-01" @default.
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- W2091873855 title "Pyrimidine benzamide-based thrombopoietin receptor agonists" @default.
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- W2091873855 doi "https://doi.org/10.1016/j.bmcl.2007.07.038" @default.
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