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合成具有 4-甲氧基萘环的 1,3,4-噁二唑类化合物:发现具有抗菌活性的新化合物。

Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity.

机构信息

Chemistry Department, State University of Maringá, PR, 87020-900, Brazil.

Department of Clinical Analysis & Biomedicine, Laboratory of Medical Mycology, State University of Maringá, Maringá, PR, 87020-900, Brazil.

出版信息

Future Med Chem. 2023 Dec;15(24):2239-2255. doi: 10.4155/fmc-2023-0153. Epub 2023 Nov 28.

Abstract

Paracoccidioidomycosis (PCM) is a systemic infection caused by spp. (). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, caused by (). Futhermore, the long treatment time of TB and PCM and the cases of TB drug resistance impose difficulties for the cure of these diseases. New 1,3,4-oxadiazoles containing the 4-methoxynaphthalene ring were synthesized and their antimicrobial activity was evaluated against and . The derivative (with 2-hydroxy-5-nitrophenyl subunit) is the most promising of the series. The 1,3,4-oxadiazole can be used as a prototype drug candidate, with anti- and anti- activities, showing a broad-spectrum profile for the treatment of both pulmonary infections.

摘要

球孢子菌病(PCM)是一种由 spp.()引起的系统性感染。PCM 可与另一种肺部感染结核分枝杆菌(TB)相关或临床混淆,由 ()引起。此外,TB 和 PCM 的长期治疗时间以及 TB 耐药病例给这些疾病的治愈带来了困难。 合成了含有 4-甲氧基萘环的新型 1,3,4-噁二唑类化合物,并评估了它们对 和 的抗菌活性。衍生物 (具有 2-羟基-5-硝基苯基亚基)是该系列中最有前途的化合物。 1,3,4-噁二唑 可作为一种原型候选药物,具有抗 和 活性,对两种肺部感染均显示出广谱特性。

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