Synthesis and in vitro selective anti-Helicobacter pylori activity of pyrazoline derivatives
- 作者：Chimenti ; F. ; Bizzarri ; B. ; Manna ; F. ; Bolasco ; A. ; Secci ; D. ; Chimenti ; P. ; Granese ; A. ; Rivanera ; D. ; et. al.
- 关键词：Pyrazoline ; Antibacterial activity ; Anti-Helicobacter pylori activity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2005
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：February 1, 2005
- 卷：15
- 期：3
- 页码：603-607
- 文件大小：282 K
摘要
In order to develop new anti-Helicobacter pylori agents, a series of N1-substituted 3,5-diphenyl pyrazolines P1芒芒芒P13 was prepared and evaluated for their antibacterial activity. All synthesized compounds showed little or no activity against different species of Gram-positive and Gram-negative bacteria of clinical relevance and against various strains of pathogenic fungi. The same derivatives exhibited a significant degree of activity against a range of H. pylori strains, including those resistant to the reference compound metronidazole. Among the prepared compounds those with an N1-acetyl group and a 4-methoxy substituent in the 5-phenyl ring showed the best activity against H. pylori metronidazole resistant strains in the 1芒芒芒4芒芒g/mL MIC range.