Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, Sandwich, Kent CT13 9NJ, United Kingdom.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1156-9. doi: 10.1016/j.bmcl.2011.11.098. Epub 2011 Dec 1.
This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine H4 receptor antagonist with moderate clearance and a high volume of distribution.
这封信描述了一系列基于八氢吡咯并[3,4-c]吡咯的选择性组氨酸 hH4 受体拮抗剂的发现和合成。酰胺化合物 20 被发现是一种有效的、选择性的组胺 H4 受体拮抗剂,具有中等的清除率和高分布容积。