| Literature DB >> 19186055 |
Michael J Munchhof1, Amy S Antipas, Laura C Blumberg, William H Brissette, Matthew F Brown, Jeffrey M Casavant, Jonathan L Doty, James Driscoll, Thomas M Harris, Lilli A Wolf-Gouveia, Christopher S Jones, Qifang Li, Robert G Linde, Paul D Lira, Anthony Marfat, Eric McElroy, Mark Mitton-Fry, Sandra P McCurdy, Lawrence A Reiter, Sharon L Ripp, Andrei Shavnya, Lisa M Thomasco, Kristen A Trevena.
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.Entities:
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Year: 2009 PMID： 19186055 DOI： 10.1016/j.bmcl.2009.01.032
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823