| Autor: |
Yoshida, Yoshiki, Barrett, David, Azami, Hidenori, Morinaga, Chizu, Matsumoto, Satoru, Matsumoto, Yoshimi, Takasugi, Hisashi |
| Zdroj: |
Bioorganic & Medicinal Chemistry; November 1999, Vol. 7 Issue: 11 p2647-2666, 20p |
| Abstrakt: |
The synthesis and optimization of the anti-Helicobacter pyloriactivity of a novel series of benzyloxyisoquinoline derivatives that was discovered by a random screening process, are described. In the in vitro assay, compound 10ccontaining a 3-acetamido-2,6-dichlorobenzyl substituent was found to have extremely potent activity against H. pyloriand no activity against other common bacteria. The anti-H. pyloriactivity of 10cwas superior to that of amoxicillin (AMPC) (1) and clarithromycin (CAM) (2). However, 10cdid not show in vivo efficacy in a mouse infection model; a feature attributed to the lack of strong bactericidal activity at short contact times. |
| Databáze: |
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