通过骨架跃迁发现新型吲哚系列EP1受体拮抗剂。
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
作者信息
Hall Adrian, Billinton Andy, Brown Susan H, Chowdhury Anita, Giblin Gerard M P, Goldsmith Paul, Hurst David N, Naylor Alan, Patel Sadhana, Scoccitti Tiziana, Theobald Pamela J
机构信息
Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.
出版信息
Bioorg Med Chem Lett. 2008 Apr 15;18(8):2684-90. doi: 10.1016/j.bmcl.2008.03.018. Epub 2008 Mar 10.
We describe the medicinal chemistry approach that generated a novel indole series of EP(1) receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.
我们描述了生成新型吲哚类EP(1)受体拮抗剂的药物化学方法。对这个新模板的构效关系进行了评估，最终确定了化合物12g，它在炎症性疼痛的临床前模型中显示出体内疗效。
Zotero 插件