10.1021/jm060657g.s001
Trond Ulven
Trond
Ulven
Jean-Marie Receveur
Jean-Marie
Receveur
Marie Grimstrup
Marie
Grimstrup
Øystein Rist
Øystein
Rist
Thomas M. Frimurer
Thomas M.
Frimurer
Lars-Ole Gerlach
Lars-Ole
Gerlach
Jesper Mosolff Mathiesen
Jesper Mosolff
Mathiesen
Evi Kostenis
Evi
Kostenis
Lena Uller
Lena
Uller
Thomas Högberg
Thomas
Högberg
Novel Selective Orally Active CRTH2 Antagonists
for Allergic Inflammation Developed from in
Silico Derived Hits
American Chemical Society
2006
CRTH 2
CRTH 2 Antagonists
ADME
Silico Derived HitsHits
mucus cell hyperplasia
novel compound class
2006-11-16 00:00:00
Journal contribution
https://acs.figshare.com/articles/journal_contribution/Novel_Selective_Orally_Active_CRTH2_Antagonists_for_Allergic_Inflammation_Developed_from_in_Silico_Derived_Hits/3047260
Hits from an in silico derived focused library for CRTH2
were transformed into highly selective antagonists with favorable
ADME properties. Oral administration of 4-bromo-2-(1-phenyl-1<i>H</i>-pyrazole-4-carbonyl)phenoxyacetic acid (<b>19</b>) inhibited peribronchial
eosinophilia and mucus cell hyperplasia in a mouse model of allergic
asthma, supporting the therapeutic potential of this novel compound
class. In addition, this selective pharmacological tool compound
provides further evidence for CRTH2 as a relevant therapeutic target
for treatment of Th2- and eosinophil-related inflammation.