Bioorganic & Medicinal Chemistry Letters 2010-10-01

Novel pyrimidines as acid pump antagonists (APAs).

Young Ae Yoon, Chan Sun Park, Myung Hun Cha, Hyunho Choi, Jae Young Sim, Jae Gyu Kim

Index: Bioorg. Med. Chem. Lett. 20(19) , 5735-8, (2010)

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Abstract

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.Copyright © 2010 Elsevier Ltd. All rights reserved.