咪唑并[1,2-a]嘧啶新衍生物的合成和抗霉菌活性。

IF 2.2 4区化学 Q2 CHEMISTRY, ORGANIC

Beilstein Journal of Organic Chemistry Pub Date : 2024-11-05 eCollection Date: 2024-01-01 DOI:10.3762/bjoc.20.236

Dmitriy Yu Vandyshev, Daria A Mangusheva, Khidmet S Shikhaliev, Kirill A Scherbakov, Oleg N Burov, Alexander D Zagrebaev, Tatiana N Khmelevskaya, Alexey S Trenin, Fedor I Zubkov

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引用次数: 0

摘要

通过现成的 2-氨基咪唑与 N-取代马来酰亚胺或 N-芳基紫苏酰亚胺的相互作用，以令人满意的收率形成了咪唑并[1,2-a]嘧啶的杂环核心。根据实验数据、反应混合物的 HPLC-MS 分析和量子化学计算，推测了所研究过程的机理。所得咪唑并[1,2-a]嘧啶与已在临床上使用的药物伏立康唑的分子对接结果表明，它们可能对白色念珠菌具有抗真菌活性。

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Synthesis and antimycotic activity of new derivatives of imidazo[1,2-a]pyrimidines.

The heterocyclic core of imidazo[1,2-a]pyrimidine was formed in satisfactory yields as a result of the interaction of the readily available 2-aminoimidazole with N-substituted maleimides or N-arylitaconimides. The mechanism of the studied processes was postulated basing on experimental data, HPLC-MS analysis of reaction mixtures, and quantum chemical calculations. Molecular docking results of the obtained imidazo[1,2-a]pyrimidines, when compared with voriconazole, a drug already in clinical use, suggest that they may possess antifungal activity against Candida albicans.

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来源期刊

Beilstein Journal of Organic Chemistry 化学-有机化学

CiteScore

4.90

自引率

3.70%

发文量

167

审稿时长

1.4 months

期刊介绍： The Beilstein Journal of Organic Chemistry is an international, peer-reviewed, Open Access journal. It provides a unique platform for rapid publication without any charges (free for author and reader) – Platinum Open Access. The content is freely accessible 365 days a year to any user worldwide. Articles are available online immediately upon publication and are publicly archived in all major repositories. In addition, it provides a platform for publishing thematic issues (theme-based collections of articles) on topical issues in organic chemistry. The journal publishes high quality research and reviews in all areas of organic chemistry, including organic synthesis, organic reactions, natural product chemistry, structural investigations, supramolecular chemistry and chemical biology.