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2026 202604026

DOI: https://doi.org/10.6023/cjoc202604026

研究论文

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
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  • 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

  网络出版日期: 2026-09-08

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.

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

  • Lu Jiaqi ,
  • Zhang Lei ,
  • Zhang Ping
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  • aCollege of Chemistry and Materials Science, Hebei Normal University, Shijiazhuang 050024

Received date: 2026-04-17

  Revised date: 2026-06-24

  Online published: 2026-09-08

Supported by

National Natural Science Foundation of China (No.21801059) and the Technology Innovation Fundation of Hebei Normal University (L2019K02).

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摘要

为探寻更优异抑真菌活性的新颖化合物,在保留原有活性基团的基础上,通过药效团拼合策略,设计合成了同时含有噻吩和三氮唑杂环取代的1,5-苯并硫氮杂䓬Ⅱ'a~Ⅱ'e.在合成系列1,5-苯并硫氮杂䓬化合物VIa~VIe时,意外得到了2-噻吩亚甲基取代的新型1,5-苯并硫氮杂䓬Ⅶa~Ⅶe,提出了Ⅶa~Ⅶe生成的可能历程.测试了目标物Ⅱ'a~Ⅱ'e和Ⅶa~Ⅶe的抑真菌活性：Ⅱ'a~Ⅱ'e对新生隐球菌和白色念珠菌有中度的抑制作用,Ⅶa~Ⅶe有轻到中度的抑制作用,其中Ⅱ'a和Ⅶb对白色念珠菌展现出相对更优的活性,这一发现为抗真菌药物的结构优化提供了初步线索.

关键词： 杂环化合物; 1,5-苯并硫氮杂䓬; 抑真菌活性

本文引用格式

鲁佳琪 , 张磊 , 张萍 . 杂环取代的1,5-苯并硫氮杂䓬的合成及抑真菌活性[J]. 有机化学, 2026 : 202604026 . DOI: 10.6023/cjoc202604026

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

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