Anti-Helicobacter pylori agents endowed with H2-antagonist properties.
New anti-Helicobacter pylori (H. pylori) agents endowed with H2-antagonists properties were obtained by combining the lamtidine derived pharmacophoric group with the antibiotic calvatic acid. All the compounds were tested for their irreversible H2-antagonist properties and for their ability to inhibit 20 H. pylori strains, two of them metronidazole resistant. The most active derivative (compound 4) displayed antimicrobial activity similar to metronidazole.
Sorba
G
G
Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università degli Studi del Piemonte Orientale, Novara, Italy.
Bertinaria
M
M
Di Stilo
A
A
Gasco
A
A
Scaltrito
M M
MM
Brenciaglia
M I
MI
Dubini
F
F
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D001667:Binding, Competitive; D020650:Combinatorial Chemistry Techniques; D004305:Dose-Response Relationship, Drug; D004351:Drug Resistance; D006168:Guinea Pigs; D006325:Heart Atria / Q000737:chemistry; D016480:Helicobacter pylori / Q000187:drug effects*; D006632:Histamine / Q000378:metabolism; D006635:Histamine H2 Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D008795:Metronidazole / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D011970:Receptors, Histamine H2 / Q000378:metabolism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D001565:Benzoates; D006635:Histamine H2 Antagonists; D009570:Nitriles; D010880:Piperidines; D011970:Receptors, Histamine H2; D014230:Triazoles; D008795:Metronidazole; C010057:calvatic acid; D006632:Histamine; C038304:lamtidine