Discovery Chemistry, Pfizer Global Research and Development, Sandwich, United Kingdom.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2224-8. doi: 10.1016/j.bmcl.2010.02.018. Epub 2010 Feb 8.
A series of amides were investigated as potential bioisosteres of previously reported triazole oxytocin antagonists. A range of potent analogues were identified, although SAR for potency and selectivity over the related V(1A) and V(2) receptors was found to be somewhat divergent from that observed for the corresponding triazole series. The high synthetic accessibility of this new amide series also facilitated the identification of a range of alternative left hand side (biaryl replacement) substituents which gave good levels of oxytocin antagonism.
研究了一系列酰胺类化合物，作为之前报道的三唑催产素拮抗剂的潜在生物等排体。虽然鉴定出了一系列有效的类似物，但与相应的三唑系列相比，其对效力和对相关 V(1A)和 V(2)受体的选择性的 SAR 发现存在一定差异。该新酰胺系列的高合成可及性还促进了一系列替代左手侧（联苯取代基）取代基的鉴定，这些取代基提供了良好的催产素拮抗作用。
