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抗幽门螺杆菌药物的结构与生物活性研究进展综述。

A review on the structures and biological activities of anti-Helicobacter pylori agents.

机构信息

Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Department of Organic Chemistry, Faculty of Chemistry, University of Mazandaran, Babolsar, Iran.

出版信息

Eur J Med Chem. 2021 Nov 5;223:113669. doi: 10.1016/j.ejmech.2021.113669. Epub 2021 Jun 23.

Abstract

Helicobacter pylori is one of the main causal risk factor in the generation of chronic gastritis, gastroduodenal ulcers and gastric carcinoma. Thus, the eradication of H. pylori infection is an important way for preventing and managing the gastric diseases. Multiple-therapy with several antibacterial agents is used for the eradication of H. pylori infections; however the increase of resistance to H. pylori strains has resulted in unsatisfactory eradication and unsuccessful treatment. Furthermore, the combination therapy with high dosing leads to the disruption of intestinal microbial flora and undesired side effects. Therefore, the search for new therapeutic agents with high selectivity against H. pylori is a field of current interest. In recent years, diverse compounds originating from natural sources or synthetic drug design programs were evaluated and tried to optimize for applying against H. pylori. In this review, we have described various classes of anti-H. pylori compounds, their structure-activity relationship studies, and mechanism of actions, which could be useful for the development of new drugs for the treatment of H. pylori infections.

摘要

幽门螺杆菌是导致慢性胃炎、胃十二指肠溃疡和胃癌的主要致病风险因素之一。因此,根除幽门螺杆菌感染是预防和治疗胃部疾病的重要方法。多种抗菌药物联合治疗用于根除幽门螺杆菌感染;然而,幽门螺杆菌菌株耐药性的增加导致根除效果不理想和治疗失败。此外,高剂量联合治疗会破坏肠道微生物菌群并产生不良副作用。因此,寻找对幽门螺杆菌具有高选择性的新型治疗药物是当前的研究热点。近年来,人们对来源于天然来源或药物设计方案的多种化合物进行了评估,并尝试对其进行优化,以应用于治疗幽门螺杆菌。在本文中,我们描述了各种抗幽门螺杆菌化合物的类别、它们的构效关系研究和作用机制,这对于开发治疗幽门螺杆菌感染的新药可能是有用的。

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