Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom.
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1851-3. doi: 10.1016/j.bmcl.2010.01.143. Epub 2010 Feb 2.
A series of azetidine ureas were investigated as potential bioisosteres of previously reported azetidinyltriazole oxytocin antagonists. Although potency was somewhat reduced in several close-in analogues, one compound, 9, was both a potent oxytocin antagonist and demonstrated significant selectivity over the closely related vasopressin V(1A) receptor.
研究了一系列氮杂环丁烷脲作为先前报道的氮杂环丁烷三唑催产素拮抗剂的潜在生物等排体。尽管在几个紧邻的类似物中，活性有所降低，但有一种化合物 9 既是一种有效的催产素拮抗剂，又对密切相关的血管加压素 V(1A)受体表现出显著的选择性。
