Yuhan Research Institute, 416-1 Gongse-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-902, Republic of Korea.
Bioorg Med Chem Lett. 2010 Oct 1;20(19):5735-8. doi: 10.1016/j.bmcl.2010.08.007. Epub 2010 Aug 6.
A series of pyrimidine derivatives as acid pump antagonists (APAs) was synthesized and the inhibitory activities against H(+)/K(+) ATPase isolated from hog gastric mucosa were determined. After elaborating on substituents at C2 and C4 position of the pyrimidine scaffold, we have observed that the compound 7h is a potent APA with H(+)/K(+) ATPase, IC(50) = 52 nM.
我们合成了一系列嘧啶衍生物作为酸泵拮抗剂（APAs），并测定了它们对猪胃黏膜分离的 H(+)/K(+)ATP 酶的抑制活性。在详细研究了嘧啶支架的 C2 和 C4 位置的取代基后，我们发现化合物 7h 是一种具有强抑制活性的 APA，其对 H(+)/K(+)ATP 酶的半数抑制浓度（IC(50)）为 52nM。
