Biswas Kaustav, Aya Toshihiro, Qian Wenyuan, Peterkin Tanya A N, Chen Jian Jeffrey, Human Jason, Hungate Randall W, Kumar Gondi, Arik Leyla, Lester-Zeiner Dianna, Biddlecome Gloria, Manning Barton H, Sun Hong, Dong Hong, Huang Ming, Loeloff Richard, Johnson Eileen J, Askew Benny C
Department of Chemistry Research and Discovery, Amgen Inc., One Amgen Center Drive, MS 29-1-B, Thousand Oaks, CA 91320, USA.
Bioorg Med Chem Lett. 2008 Sep 1;18(17):4764-9. doi: 10.1016/j.bmcl.2008.07.108. Epub 2008 Jul 31.
We report the development of aryl sulfones as Bradykinin B1 receptor antagonists. Variation of the linker region identified diol 23 as a potent B1 antagonist, while modifications of the aryl moiety led to compound 26, both of which were efficacious in rabbit biochemical challenge and pain models.
我们报道了芳基砜类化合物作为缓激肽B1受体拮抗剂的研发情况。连接区域的变化确定二醇23为一种有效的B1拮抗剂，而芳基部分的修饰则产生了化合物26，这两种化合物在兔生化激发试验和疼痛模型中均有效。
