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ID: ALA1152884
Journal: Bioorg Med Chem Lett
Title: The identification of orally bioavailable thrombopoietin agonists.
Authors: Munchhof MJ, Antipas AS, Blumberg LC, Brissette WH, Brown MF, Casavant JM, Doty JL, Driscoll J, Harris TM, Wolf-Gouveia LA, Jones CS, Li Q, Linde RG, Lira PD, Marfat A, McElroy E, Mitton-Fry M, McCurdy SP, Reiter LA, Ripp SL, Shavnya A, Thomasco LM, Trevena KA.
Abstract: Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor agonists. Unfortunately, the structural features required for the desired activity conferred physicochemical properties that were not favorable for the development of an oral agent. The physical properties of the series were improved by replacing the aminopyrimidinyl group with a piperidine-4-carboxylic acid moiety. The resulting compounds possessed favorable in vivo pharmacokinetic properties, including good bioavailability.
CiteXplore: 19186055