Synthesis and Antifungal Activity of Heterocyclic Substituted 1,5-Benzothiazepines

doi:10.6023/cjoc202604026

Chinese Journal of Organic Chemistry Previous Articles Next Articles

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杂环取代的1,5-苯并硫氮杂䓬的合成及抑真菌活性

鲁佳琪, 张磊, 张萍^*

^a河北师范大学化学与材料科学学院石家庄 050024

收稿日期:2026-04-17 修回日期:2026-06-24
基金资助:
国家自然科学基金(No.21801059)及河北师范大学技术创新基金（L2019K02）资助项目.

Synthesis and Antifungal Activity of Heterocyclic Substituted 1,5-Benzothiazepines

Lu Jiaqi, Zhang Lei, Zhang Ping^*

^aCollege of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024

Received:2026-04-17 Revised:2026-06-24
Contact: *E-mail: zhangpingp@sina.com
Supported by:
National Natural Science Foundation of China (No.21801059) and the Technology Innovation Fundation of Hebei Normal University (L2019K02).

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Abstract

In order to find novel compounds with superior antifungal activity, a series of 1,5-benzothiazepines II'a~II'e containing both thiophene and triazole heterocyclic substitutions were designed and synthesized while retaining the original active groups by a pharmacophore hybridization strategy. During the synthesis of the 1,5-benzothiazepines VIa~VIe, a novel 1,5-benzothiazepines VIIa~VIIe with 2-thiophene methylene substitution were unexpectedly obtained, and a possible mechanism for the formation of VIIa~VIIe was proposed. The antifungal activities of II'a~II'e and VIIa~VIIe were tested: II'a~II'e showed moderate inhibitory effects on C. neoformans and C. albicans, while VIIa~VIIe showed mild to moderate inhibitory effects. Among them, II'a and VIIb exhibited relatively better activity against C. albicans, providing preliminary clues for the structural optimization of antifungal drugs.

Key words: heterocyclic compound, 1,5-benzothiazepine, antifungal activity

Cite this article

Lu Jiaqi, Zhang Lei, Zhang Ping. Synthesis and Antifungal Activity of Heterocyclic Substituted 1,5-Benzothiazepines[J]. Chinese Journal of Organic Chemistry, doi: 10.6023/cjoc202604026.

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杂环取代的1,5-苯并硫氮杂䓬的合成及抑真菌活性

Synthesis and Antifungal Activity of Heterocyclic Substituted 1,5-Benzothiazepines

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