Studies on anti-Helicobacter pylori agents.: Part 1:: Benzyloxyisoquinoline derivatives

被引：27

作者：

Yoshida, Y

Barrett, D

Azami, H

Morinaga, C

Matsumoto, S

Matsumoto, Y

Takasugi, H

机构：

[1] Fujisawa Pharmaceut Co Ltd, Intellectual Property Div, Med Chem Res Labs, Yodogawa Ku, Osaka 5328514, Japan

[2] Fujisawa Pharmaceut Co Ltd, Med Biol Res Labs, Yodogawa Ku, Osaka 5328514, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 11期

关键词：

D O I：

10.1016/S0968-0896(99)00203-5

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives that was discovered by a random screening process, are described. In the in vitro assay, compound 10c containing a 3-acetamido-2,6-dichlorobenzyl substituent was found to have extremely potent activity against H. pylori and no activity against other common bacteria. The anti-H. pylori activity of 10c was superior to that of amoxicillin (AMPC) (1) and clarithromycin (CAM) (2), However, 10c did not show in vivo efficacy in a mouse infection model; a feature attributed to the lack of strong bactericidal activity at short contact times. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：2647 / 2666

页数：20

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