2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
High throughput screening identified a phenoxyacetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a compound with functional potency for inhibition of human eosinophil shape change and oral bioavailability in the rat.
Sandham
David A
DA
Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK. david.sandham@novartis.com
Aldcroft
Clive
C
Baettig
Urs
U
Barker
Lucy
L
Beer
David
D
Bhalay
Gurdip
G
Brown
Zarin
Z
Dubois
Gerald
G
Budd
David
D
Bidlake
Louise
L
Campbell
Emma
E
Cox
Brian
B
Everatt
Brian
B
Harrison
David
D
Leblanc
Catherine J
CJ
Manini
Jodie
J
Profit
Rachael
R
Stringer
Rowan
R
Thompson
Katy S
KS
Turner
Katharine L
KL
Tweed
Morris F
MF
Walker
Christoph
C
Watson
Simon J
SJ
Whitebread
Steven
S
Willis
Jennifer
J
Williams
Gareth
G
Wilson
Caroline
C
D000085:Acetates / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001682:Biological Availability; D004804:Eosinophils / Q000187:drug effects; D006801:Humans; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D000085:Acetates; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor; C415326:phenoxyacetic acid