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设计具有抗生物膜活性的非细胞毒性 6,7-二羟基香豆素-5-羧酸酯,针对 和 。

Design of non-cytotoxic 6,7-dihydroxycoumarin-5-carboxylates with antibiofilm activity against and .

机构信息

Institute of Organic Chemistry, Technische Universität Braunschweig, Hagenring 30, 38106 Braunschweig, Germany.

Laboratories of Natural Product and Conjugation Chemistry (naconLabs) - A Technology Transfer Center of iTUBS mbH, Wilhelmsgarten 3, 38100 Braunschweig, Germany.

出版信息

Org Biomol Chem. 2023 Jun 14;21(23):4744-4749. doi: 10.1039/d3ob00303e.

Abstract

The 6,7-dihydroxycoumarin-5-carboxylates DHCou and 4-Me-DHCou have been synthesized five-step route including a propargyl-Claisen rearrangement as key step. The compounds show antibiofilm activity against and but lack the cytotoxic activity of parent 6,7-dihydroxycoumarines such as esculetin and 4-methylesculetin.

摘要

6,7-二羟基香豆素-5-羧酸酯 DHCou 和 4-Me-DHCou 已通过包括炔丙基-Claisen 重排在内的五步路线合成,该重排是关键步骤。这些化合物对 和 具有抗生物膜活性,但缺乏母体 6,7-二羟基香豆素(如秦皮素和 4-甲氧基秦皮素)的细胞毒性。

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