Nitrogen-containing heterocyclic drug products approved by the FDA in 2023: Synthesis and biological activity,European Journal of Medicinal Chemistry

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Nitrogen-containing heterocyclic drug products approved by the FDA in 2023: Synthesis and biological activity
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2024-09-06 , DOI: 10.1016/j.ejmech.2024.116838
Weijiang Luo ₁ , Yiqi Liu ₁ , Hui Qin ₂ , Zeyan Zhao ₁ , Suqi Wang ₁ , Weimin He ₃ , Shengsong Tang ₄ , Junmei Peng ₁

Affiliation

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.

中文翻译：

FDA 于 2023 年批准的含氮杂环药品：合成和生物活性

本文介绍了 13 年美国食品药品监督管理局（FDA）新批准的 2023 种含氮杂环药物。这些药物针对多种治疗领域，包括 IgA 肾病患者的蛋白尿、成人偏头痛、Rett 综合征、PI3Kδ 综合征、血管舒缩症状、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具有常见的芳香族杂环化合物，如吡咯、咪唑、吡唑、异恶唑、吡啶和嘧啶，以及脂肪族杂环化合物，如己内酰胺、哌嗪和哌啶。一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。本文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。

更新日期：2024-09-06

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