7-(2-氨基烷基)吗啉代喹诺酮类作为抗幽门螺杆菌药物的合成及构效关系

Synthesis and structure-activity relationships of 7-(2-aminoalkyl)morpholinoquinolones as anti-Helicobacter pylori agents.

作者信息

Sakurai N, Sano M, Hirayama F, Kuroda T, Uemori S, Moriguchi A, Yamamoto K, Ikeda Y, Kawakita T

机构信息

Research Laboratory Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2185-90. doi: 10.1016/s0960-894x(98)00390-4.

DOI:10.1016/s0960-894x(98)00390-4

PMID:9873510

Abstract

A series of the titled compounds was synthesized and tested for anti-Helicobacter pylori activities. We discovered Y-34867 having the most potent activity against Helicobacter pylori among the quinolones tested along with high photostability. Furthermore, Y-34867 showed an excellent therapeutic effect in the experimental Helicobacter pylori infected Mongolian gerbil model.

摘要

合成了一系列标题化合物，并测试了它们的抗幽门螺杆菌活性。我们发现Y-34867在测试的喹诺酮类化合物中对幽门螺杆菌具有最强的活性，同时具有高光稳定性。此外，Y-34867在实验性幽门螺杆菌感染的蒙古沙鼠模型中显示出优异的治疗效果。