抗米根霉药坦桑酸A的构效关系研究。

IF 2.2 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-07-16 DOI:10.1016/j.bmcl.2025.130343

Kotaro Tanaka , Shiho Arima , Daiki Lee , Satoshi Ohte , Hiroshi Tomoda , Ryuji Uchida , Taichi Ohshiro , Tohru Nagamitsu

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引用次数: 0

摘要

本研究旨在通过对坦桑酸A （TZAA）的构效关系研究，为开发治疗毛霉病感染的有效抗真菌药物提供依据。为此，合成了新的具有侧链和/或c8 -甲基基团修饰的TZAA类似物。这些类似物无法从天然的TZAA中获得，因此需要全合成。结果表明，四种新合成的TZAA类似物比TZAA对稻瘟病菌表现出更强的选择性抑制活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Structure–activity relationship studies of tanzawaic acid A, an antifungal agent against Rhizopus oryzae

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Structure–activity relationship studies of tanzawaic acid A, an antifungal agent against Rhizopus oryzae

Through structure–activity relationship studies of tanzawaic acid A (TZAA), this research aims to contribute the development of potent antifungal drugs for treating mucormycosis infections. To this end, new TZAA analogs bearing chemical modifications in the side chain and/or C8-methyl group moieties were synthesized. These analogs are not accessible from natural TZAA and therefore required total synthesis. As a result, four of the newly synthesized TZAA analogs exhibited more potent and selective inhibitory activity against R. oryzae compared to TZAA.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.