2023 年美国 FDA 批准的含氮杂环药物产品:合成与生物活性

IF 6 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2024-09-06 DOI:10.1016/j.ejmech.2024.116838
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引用次数: 0

摘要

本文介绍了美国食品和药物管理局(FDA)在 2023 年新批准的 13 种含氮杂环药物。这些药物针对多个治疗领域,包括 IgA 肾病患者的蛋白尿、成人偏头痛、Rett 综合征、PI3Kδ 综合征、血管运动症状、斑秃、急性髓性白血病、产后抑郁症、骨髓纤维化以及各种癌症和肿瘤类型。这些获批药物的分子结构以常见的芳香杂环化合物(如吡咯、咪唑、吡唑、异噁唑、吡啶和嘧啶)以及脂肪杂环化合物(如己内酰胺、哌嗪和哌啶)为特征。有些化合物还含有多个杂原子,如 1,2,4-噻二唑和 1,2,4-三唑。文章全面概述了每种化合物的生物活性谱、药物化学发现和合成方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Nitrogen-containing heterocyclic drug products approved by the FDA in 2023: Synthesis and biological activity

This article profiles 13 newly approved nitrogen-containing heterocyclic drugs by the U.S. Food and Drug Administration (FDA) in 2023. These drugs target a variety of therapeutic areas including proteinuria in patients with IgA nephropathy, migraine in adults, Rett syndrome, PI3Kδ syndrome, vasomotor symptoms, alopecia areata, acute myeloid leukemia, postpartum depression, myelofibrosis, and various cancer and tumor types. The molecular structures of these approved drugs feature common aromatic heterocyclic compounds such as pyrrole, imidazole, pyrazole, isoxazole, pyridine, and pyrimidine, as well as aliphatic heterocyclic compounds like caprolactam, piperazine, and piperidine. Some compounds also contain multiple heteroatoms like 1,2,4-thiadiazole and 1,2,4-triazole. The article provides a comprehensive overview of the bioactivity spectrum, medicinal chemistry discovery, and synthetic methods for each compound.

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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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