Structure-activity relationships and hepatic safety risks of thiazole agonists of the thrombopoietin receptor.
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.
Antipas
Amy S
AS
Pfizer Worldwide Research and Development, Groton, CT 06340, USA.
Blumberg
Laura C
LC
Brissette
William H
WH
Brown
Matthew F
MF
Casavant
Jeffrey M
JM
Doty
Jonathan L
JL
Driscoll
James
J
Harris
Thomas M
TM
Jones
Christopher S
CS
McCurdy
Sandra P
SP
McElroy
Eric
E
Mitton-Fry
Mark
M
Munchhof
Michael J
MJ
Reim
David A
DA
Reiter
Lawrence A
LA
Ripp
Sharon L
SL
Shavnya
Andrei
A
Smeets
Marc I
MI
Trevena
Kristen A
KA
D000818:Animals; D008099:Liver / Q000187:drug effects* / Q000378:metabolism; D053628:Receptors, Thrombopoietin / Q000819:agonists*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*
D053628:Receptors, Thrombopoietin; D013844:Thiazoles