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氨基甲酸酯基团作为药物中的结构基序:用作治疗剂的氨基甲酸酯衍生物综述。

Carbamate group as structural motif in drugs: a review of carbamate derivatives used as therapeutic agents.

机构信息

Institute for Medical Research and Occupational Health, Zagreb, Croatia.

出版信息

Arh Hig Rada Toksikol. 2020 Dec 31;71(4):285-299. doi: 10.2478/aiht-2020-71-3466.

DOI:10.2478/aiht-2020-71-3466
PMID:33410773
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7968508/
Abstract

Due to their very good chemical and proteolytic stability, ability to penetrate cell membranes, and resemblance to a peptide bond, carbamate derivatives have received much attention in recent years and got an important role in modern drug discovery and medicinal chemistry. Today, carbamates make structural and/or functional part of many drugs and prodrugs approved and marketed for the treatment of various diseases such as cancer, epilepsy, hepatitis C, HIV infection, and Alzheimer's disease. In drugs they can play a role in drug-target interaction or improve the biological activity of parent molecules. In prodrugs they are mainly used to delay first-pass metabolism and enhance the bioavailability and effectiveness of compounds. This brief review takes a look at the properties and use of carbamates in various fields of medicine and provides quick insights into the mechanisms of action for some of them.

摘要

由于其极好的化学和蛋白水解稳定性、穿透细胞膜的能力以及与肽键的相似性,近年来氨基甲酸酯衍生物受到了广泛关注,并在现代药物发现和药物化学中发挥了重要作用。如今,氨基甲酸酯已成为许多已批准上市用于治疗各种疾病(如癌症、癫痫、丙型肝炎、HIV 感染和老年痴呆症)的药物和前药的结构和/或功能部分。在药物中,它们可以在药物-靶标相互作用中发挥作用,或提高母体分子的生物活性。在前药中,它们主要用于延迟首过代谢,提高化合物的生物利用度和疗效。这篇简要综述考察了氨基甲酸酯在医学各个领域的性质和用途,并快速了解了其中一些的作用机制。

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