具有H2拮抗剂特性的抗幽门螺杆菌药物。

Anti-Helicobacter pylori agents endowed with H2-antagonist properties.

作者信息

Sorba G, Bertinaria M, Di Stilo A, Gasco A, Scaltrito M M, Brenciaglia M I, Dubini F

机构信息

Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche, Università degli Studi del Piemonte Orientale, Novara, Italy.

出版信息

Bioorg Med Chem Lett. 2001 Feb 12;11(3):403-6. doi: 10.1016/s0960-894x(00)00671-5.

DOI:10.1016/s0960-894x(00)00671-5

PMID:11212121

Abstract

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.

摘要

通过将雷尼替丁衍生的药效基团与抗生素马勃酸相结合，获得了具有H2拮抗剂特性的新型抗幽门螺杆菌（H. pylori）药物。对所有化合物进行了不可逆H2拮抗剂特性测试以及抑制20株幽门螺杆菌菌株的能力测试，其中两株对甲硝唑耐药。活性最强的衍生物（化合物4）表现出与甲硝唑相似的抗菌活性。