title: Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.
abstract: A novel series of biaryl phenoxyacetic acids was discovered as potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A hit compound 4 was discovered from high throughput screening. Modulation of multiple aryl substituents afforded both agonists and antagonists, with small changes often reversing the mode of action. Understanding the complex SAR allowed design of potent antagonists such as potential candidate 34.
authors: Medicinal Chemistry, AstraZeneca R&D Charnwood, Loughborough, Leicestershire, UK. tim.luker@astrazeneca.com
authors: Tim
authors: T
authors: Luker
authors: Roger
authors: R
authors: Bonnert
authors: Jerzy
authors: J
authors: Schmidt
authors: Carol
authors: C
authors: Sargent
authors: Stuart W
authors: SW
authors: Paine
authors: Stephen
authors: S
authors: Thom
authors: Gary
authors: G
authors: Pairaudeau
authors: Anil
authors: A
authors: Patel
authors: Rukhsana
authors: R
authors: Mohammed
authors: Elizabeth
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authors: Akam
authors: Iain
authors: I
authors: Dougall
authors: Andrew M
authors: AM
authors: Davis
authors: Phil
authors: P
authors: Abbott
authors: Steve
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authors: Brough
authors: Ian
authors: I
authors: Millichip
authors: Thomas
authors: T
authors: McInally