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7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists |
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| Authors: | David A. Sandham Claire Adcock Kamlesh Bala Lucy Barker Zarin Brown Gerald Dubois David Budd Brian Cox Robin A. Fairhurst Markus Furegati Catherine Leblanc Jodie Manini Rachael Profit John Reilly Rowan Stringer Alfred Schmidt Katharine L. Turner Simon J. Watson Jennifer Willis Gareth Williams Caroline Wilson |
| Affiliation: | 1. Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom;2. Respiratory Diseases Area, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom;3. Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Postfach CH-4002, Basel, Switzerland |
| Abstract: | High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat. |
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