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Merck

2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.

Bioorganic & medicinal chemistry letters (2007-05-29)
David A Sandham, Clive Aldcroft, Urs Baettig, Lucy Barker, David Beer, Gurdip Bhalay, Zarin Brown, Gerald Dubois, David Budd, Louise Bidlake, Emma Campbell, Brian Cox, Brian Everatt, David Harrison, Catherine J Leblanc, Jodie Manini, Rachael Profit, Rowan Stringer, Katy S Thompson, Katharine L Turner, Morris F Tweed, Christoph Walker, Simon J Watson, Steven Whitebread, Jennifer Willis, Gareth Williams, Caroline Wilson
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
4-Chloro-2-methylphenoxyacetic acid, technical, ≥95.0% (T)
Supelco
MCPA, PESTANAL®, analytical standard
Sigma-Aldrich
Phenoxyacetic acid, 98%
Supelco
Phenoxyacetic acid, PESTANAL®, analytical standard