无水四环素衍生物的合成及抗菌研究。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-12-28 DOI:10.1016/j.bmcl.2024.130090

Yong Wang , He Wu , Guangguang Yang, Karuppu Selvaraj, Gang Chen

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引用次数: 0

摘要

由于现有四环素类药物的耐药，需要一种具有不同作用机制的新型四环素。无水四环素是一种具有独特作用机制的非常规四环素类药物，本研究综述了其合成及抗菌评价。这些衍生物包括C4-NH2， C4-OH和c9取代变体，我们的合成方法侧重于以天然四环素作为起始前体的半合成。一些C4-NH2、C4-OH和c9取代化合物的衍生物已经证明对革兰氏阳性和革兰氏阴性细菌都有有效的抗生素活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis and antibacterial study of anhydrotetracycline derivatives

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Synthesis and antibacterial study of anhydrotetracycline derivatives

A novel and new type of tetracycline with a different mechanism of action was necessary, due to the drug resistance of existing tetracyclines. This study outlines the synthesis and antibacterial evaluation of anhydro-tetracycline derivatives, which are unconventional tetracyclines with unique mechanisms of action. These derivatives include C4-NH₂, C4-OH, and C9-substituted variations, and our synthetic approach focuses on semi-synthesis using natural tetracyclines as the starting precursors. Several derivatives of C4-NH₂, C4-OH, and C9-substituted compounds have demonstrated effective antibiotic activity against both Gram-positive and Gram-negative bacteria.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.