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Nitrile-containing pharmaceuticals: target, mechanism of action, and their SAR studies
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-08-10 , DOI: 10.1039/d1md00131k Xi Wang 1 , Yuanxun Wang 2 , Xuemin Li 1 , Zhenyang Yu 1 , Chun Song 3 , Yunfei Du 1
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2021-08-10 , DOI: 10.1039/d1md00131k Xi Wang 1 , Yuanxun Wang 2 , Xuemin Li 1 , Zhenyang Yu 1 , Chun Song 3 , Yunfei Du 1
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The nitrile group is an important functional group widely found in both pharmaceutical agents and natural products. More than 30 nitrile-containing pharmaceuticals have been approved by the FDA for the management of a broad range of clinical conditions in the last few decades. Incorporation of a nitrile group into lead compounds has gradually become a promising strategy in rational drug design as it can bring additional benefits including enhanced binding affinity to the target, improved pharmacokinetic profile of parent drugs, and reduced drug resistance. This paper reviews the existing drugs with a nitrile moiety that have been approved or in clinical trials, involving their targets, molecular mechanism of pharmacology and SAR studies, and classifies them into different categories based on their clinical usages.
中文翻译：
含腈药物：靶点、作用机制及其 SAR 研究
腈基是广泛存在于药物和天然产物中的重要官能团。过去几十年来，FDA 已批准 30 多种含腈药物用于治疗多种临床病症。将腈基引入先导化合物已逐渐成为合理药物设计中一种有前景的策略，因为它可以带来额外的好处，包括增强与靶点的结合亲和力、改善母体药物的药代动力学特征以及降低耐药性。本文综述了现有已获批或处于临床试验阶段的含腈基药物，包括其作用靶点、药理学分子机制和SAR研究，并根据临床用途将其分为不同类别。
更新日期：2021-08-10
中文翻译：
含腈药物：靶点、作用机制及其 SAR 研究
腈基是广泛存在于药物和天然产物中的重要官能团。过去几十年来，FDA 已批准 30 多种含腈药物用于治疗多种临床病症。将腈基引入先导化合物已逐渐成为合理药物设计中一种有前景的策略，因为它可以带来额外的好处，包括增强与靶点的结合亲和力、改善母体药物的药代动力学特征以及降低耐药性。本文综述了现有已获批或处于临床试验阶段的含腈基药物，包括其作用靶点、药理学分子机制和SAR研究，并根据临床用途将其分为不同类别。
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