Bismuth and Helicobacter pylori

Novel Structures Derived from 2-[[(2-Pyridyl)methyl]thio]-1H-benzimidazole as Anti-Helicobacter pylori Agents, Part 1

“…Chromatography on silica (CH 2Cl2/MeOH; 19/1) and subsequent crystallization from CH2Cl2/MeCN afforded 59 mg (45%) of the title compound as a white crystalline solid (59 mg, 45%). 300 MHz 1 4-iso-Butyloxy-2-hydroxymethyl-3-methyl Pyridine (10). The title compound was prepared from 8 in two steps as described in ref 8.…”

“…More than 60% of the world's population is infected with the pathogenic, Gram-negative bacterium Helicobacter pylori. 1,2 An infection inevitably leads to gastritis, which in turn may develop into atrophy, and the pathogen has therefore been stated to be carcinogenic to humans by the World Health Organization (WHO). The bacterium is the causative agent of duodenal ulcer relapse as evidenced by numerous clinical trials, and it has been implicated in nonulcer dyspepsia and irritable bowel syndrome although firm relationships regarding these disorders are still lacking.…”

“…8 The evaluation of these sulfides in an animal model, however, suggested that their pharmacological properties were not ideal. They displayed an inherent propensity for metabolic oxidation to the corresponding sulfoxides (1), that is PPIs, and thus effectively inhibited acid secretion. While acid secretion inhibition is favorable in combination therapies together with antimicrobials, 9,10 it proved counterproductive under our monotherapy conditions.…”

Helicobacter pylori infection and peptic ulcer disease

“…Historically, the first substances in use were bismuth salts (bismuth subcitrate and bismuth sub salicylate) [66], followed by several antibiotics among the 5-nitroimidazoles, penicillins and chinolones. Antibacterial monotherapy was ineffective in the eradication of H. pylori, since such regimes typically achieved cure rates of < 20 % after 2 to 4 weeks of therapy [67].…”

“…Antibacterial monotherapy was ineffective in the eradication of H. pylori, since such regimes typically achieved cure rates of < 20 % after 2 to 4 weeks of therapy [67]. Use of mono therapy with antibiotics was eventually strongly discouraged due to the possible risk of development of antibacterial resistance [66]. The next step was the addition of a bismuth compound to metronidazole or amoxicillin that increased the overall eradication rate to approximately 50% [68].…”