Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor

Amy S Antipas; Laura C Blumberg; William H Brissette; Matthew F Brown; Jeffrey M Casavant; Jonathan L Doty; James Driscoll; Thomas M Harris; Christopher S Jones; Sandra P McCurdy; Eric McElroy; Mark Mitton-Fry; Michael J Munchhof; David A Reim; Lawrence A Reiter; Sharon L Ripp; Andrei Shavnya; Marc I Smeets; Kristen A Trevena

doi:10.1016/j.bmcl.2010.05.087

Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4069-72. doi: 10.1016/j.bmcl.2010.05.087. Epub 2010 May 26.

Affiliation

¹ Pfizer Worldwide Research and Development, Groton, CT 06340, USA.

PMID: 20558059
DOI: 10.1016/j.bmcl.2010.05.087

Abstract

5-F substitution of an aminothiazole moiety within a series of thrombopoietin receptor agonists leads to potent agents with an improved hepatic safety profile in rodent toxicology studies.

MeSH terms

Animals
Liver / drug effects*
Liver / metabolism
Receptors, Thrombopoietin / agonists*
Structure-Activity Relationship
Thiazoles / pharmacology*

Substances

Receptors, Thrombopoietin
Thiazoles