Abstract:
:In order to find a new class of anti-Helicobacter pylori (H. pylori) agents, a series of 4-[(3-acetamido)phenyl]-2-(substituted guanidino)thiazoles and some structurally rigid analoges were synthesized and evaluated for antimicrobial activity against H. pylori. Among the compounds obtained, high anti-H. pyrori activities were observed in benzyl derivative 34 (MIC = 0.025 microg/mL) and phenethyl derivatives 35 and 36 (MIC = 0.037 microg/mL and 0.017 microg/mL). Though alkyl derivatives generally showed lower activity, the 2-methoxyethyl derivative 28 preserved significant activity (MIC = 0.32 microg/mL) and also exhibited more potent gastric antisecretory activity than ranitidine. Structural restriction by bridging between the thiazole and the phenyl rings with an alkyl chain did not improve the activity in this series.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Katsura Y,Tomishi T,Inoue Y,Sakane K,Matsumoto Y,Morinaga C,Ishikawa H,Takasugi Hdoi
10.1021/jm000169nkeywords:
subject
Has Abstractpub_date
2000-08-24 00:00:00pages
3315-21issue
17eissn
0022-2623issn
1520-4804pii
jm000169njournal_volume
43pub_type
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