具有体内镇痛功效的非酸性吡唑EP1受体拮抗剂。
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
作者信息
Hall Adrian, Billinton Andy, Brown Susan H, Clayton Nicholas M, Chowdhury Anita, Giblin Gerard M P, Goldsmith Paul, Hayhow Thomas G, Hurst David N, Kilford Ian R, Naylor Alan, Passingham Barry, Winyard Lisa
机构信息
Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex, CM19 5AW, UK.
出版信息
Bioorg Med Chem Lett. 2008 Jun 1;18(11):3392-9. doi: 10.1016/j.bmcl.2008.04.018. Epub 2008 Apr 11.
Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.
在一系列先前描述的亚甲基连接的吡唑EP(1)受体拮抗剂中，羧酸基团的取代导致了酰胺、反式酰胺和氨基甲酸酯衍生物的发现。两种化合物，10a和10b，被鉴定为具有脑渗透性的化合物，并且在炎性疼痛的CFA模型中均显示出疗效。
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