Design, synthesis and anticoagulant activity evaluation of deuterium-labeled dabigatran etexilate and its intermediate derivatives

被引：0

作者：

Liang, Dawei ^{[1
]}

Wang, Chang ^{[2
]}

Ma, Yuandong ^{[2
]}

Wang, Yueqiu ^{[1
]}

Zhang, Luwen ^{[1
]}

Dong, Jinhua ^{[2
]}

机构：

[1] Yaan Polytech Coll, Sch Pharm & Med Lab Sci, Yaan 625100, Peoples R China

[2] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Peoples R China

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2025年 / 334卷 / 05期

关键词：

Dabigatran etexilate; Deuterium-labeled; Synthesis; Anticoagulant activity; DIRECT THROMBIN INHIBITOR;

D O I：

10.1007/s10967-025-10091-5

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

The deuterium-labeled dabigatran etexilate and a series of N-(4-cyanophenyl)-1-(methyl-d3)-5-carbamoyl-1H-benzo[d]imidazole-2-carbimidoyl chloride derivatives were prepared from commercially available 4-chloro-3-nitrobenzoate methyl ester as starting material and deuterium methylamine hydrochloride as the deuterium reagent. The structural properties of the intermediate derivatives were examined, and subsequently assessed for thrombin inhibition. The anticoagulant activity of the deuterium-labeled dabigatran etexilate was higher than that of unlabeled active ingredient, and most of these derivatives have certain valuable properties, which are expected to enrich the landscape of anticoagulant drug research.

引用

页码：3163 / 3172

页数：10

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