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Chinese Journal of Organic Chemistry >

2026 202604026

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

ARTICLE

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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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, 2026 : 202604026 . DOI: 10.6023/cjoc202604026

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