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含 C 末端 1-氨乙基四唑的寡肽作为新型丙氨酸消旋酶抑制剂。

C-Terminal 1-Aminoethyltetrazole-Containing Oligopeptides as Novel Alanine Racemase Inhibitors.

机构信息

Sunderland Pharmacy School, University of Sunderland, Sunderland SR1 3SD, UK.

Research & Development Microbiology, bioMérieux, 38390 La Balme-les-Grottes, France.

出版信息

Molecules. 2020 Mar 13;25(6):1315. doi: 10.3390/molecules25061315.

Abstract

In clinical culture media inoculated with patient samples, selective inhibition of commensal bacteria is essential for accurate diagnosis and effective treatment, as they can mask the presence of pathogenic bacteria. The alanine analogue, 1-aminoethyltetrazole was investigated as a potential alanine racemase inhibitor. For effective uptake and enhanced and selective antibacterial activity, a library of C-terminal 1-aminoethyltetrazole containing di- and oligopeptides were synthesized by solid phase peptide coupling techniques. The investigation of the antimicrobial activity of the synthesised compounds identified several clinically applicable selective inhibitors. These enabled differentiation between the closely related bacteria, and , which can be difficult to discriminate between in a clinical setting. In addition, differentiation between enterococci and other Gram-positive cocci was also seen.

摘要

在接种了患者样本的临床培养基中,选择性抑制共生菌对于准确诊断和有效治疗至关重要,因为它们可能掩盖病原菌的存在。丙氨酸类似物 1-氨基乙基四唑被研究为一种潜在的丙氨酸消旋酶抑制剂。为了有效摄取和增强和选择性的抗菌活性,通过固相肽偶联技术合成了含有二肽和寡肽的 C 末端 1-氨基乙基四唑的库。对合成化合物的抗菌活性的研究确定了几种临床上可应用的选择性抑制剂。这些抑制剂能够区分密切相关的细菌 和 ,在临床环境中很难区分。此外,还观察到肠球菌和其他革兰氏阳性球菌之间的分化。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4210/7145296/e6a685406348/molecules-25-01315-g001.jpg

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