2-环烷基苯氧基乙酸CRTh2受体拮抗剂
2-Cycloalkyl phenoxyacetic acid CRTh2 receptor antagonists.
作者信息
Sandham David A, Aldcroft Clive, Baettig Urs, Barker Lucy, Beer David, Bhalay Gurdip, Brown Zarin, Dubois Gerald, Budd David, Bidlake Louise, Campbell Emma, Cox Brian, Everatt Brian, Harrison David, Leblanc Catherine J, Manini Jodie, Profit Rachael, Stringer Rowan, Thompson Katy S, Turner Katharine L, Tweed Morris F, Walker Christoph, Watson Simon J, Whitebread Steven, Willis Jennifer, Williams Gareth, Wilson Caroline
机构信息
Global Discovery Chemistry, Novartis Institutes of Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, UK.
出版信息
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4347-50. doi: 10.1016/j.bmcl.2007.05.019. Epub 2007 May 13.
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.
高通量筛选确定了一种苯氧乙酸骨架作为一种新型的CRTh2受体拮抗剂化学类型，该化学类型可以进行优化，以提供一种对抑制人类嗜酸性粒细胞形态变化具有功能活性且在大鼠体内具有口服生物利用度的化合物。
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