发现取代的2,4-二甲基-（萘-4-羰基）氨基苯甲酸作为强效和选择性EP4拮抗剂。
Discovery of substituted-2,4-dimethyl-(naphthalene-4-carbonyl)amino-benzoic acid as potent and selective EP4 antagonists.
作者信息
Blanco Maria-Jesus, Vetman Tatiana, Chandrasekhar Srinivasan, Fisher Matthew J, Harvey Anita, Mudra Daniel, Wang Xu-Shan, Yu Xiao-Peng, Schiffler Matthew A, Warshawsky Alan M
机构信息
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, United States.
出版信息
Bioorg Med Chem Lett. 2016 Jan 1;26(1):105-9. doi: 10.1016/j.bmcl.2015.11.023. Epub 2015 Nov 10.
A novel series of EP4 antagonists, based on a quinoline scaffold, has been discovered. Medicinal chemistry efforts to optimize the potency of the initial hit are described. A highly potent compound in a clinically relevant human whole blood assay was identified. Selectivity and pharmacokinetic profiles of this compound are discussed.
已发现了一系列基于喹啉骨架的新型EP4拮抗剂。描述了为优化最初活性化合物的效力而进行的药物化学研究工作。在一项临床相关的人体全血试验中鉴定出了一种高效力化合物。讨论了该化合物的选择性和药代动力学特征。
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