Synthetic Approaches and Biological Significance of Four-Membered Heterocyclic Compounds.

IF 3.3 4区 医学 Q3 CHEMISTRY, MEDICINAL
Neelottama Kushwaha, Swatantra K S Kushwaha
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引用次数: 0

Abstract

A four-membered heterocycle synthesis offers a thorough exploration of these unstable organic compounds, systematically introducing the synthesis and reactions of all standard fourmembered heterocycles while showcasing various methods for creating unique variants. Due to their inherent strain, four-membered heterocyclic compounds are classified as unstable organic compounds, which makes them valuable as precursors for synthesizing a wide range of complex heterocyclic molecules. These compounds have become essential frameworks in medicinal chemistry, providing unique properties that enhance drug design and development. The incorporation of heteroatoms like nitrogen, oxygen, and sulfur into four-membered rings (such as azetidines, oxetanes, and thietanes) leads to diverse electronic, steric, and metabolic characteristics that can improve therapeutic efficacy, selectivity, and pharmacokinetics. Despite the challenges posed by their ring strain, recent advancements in chemical synthesis and functionalization techniques have made these compounds more accessible for various therapeutic applications. These strained ring structures offer increased metabolic stability, controlled lipophilicity, and the potential for advantageous binding interactions, making them suitable for multiple therapeutic uses, including oncology, infectious diseases, and CNS disorders. This review examines the key properties of four-membered heterocyclic rings, their role in drug development, recent synthetic advancements, and the potential of these compounds to yield next-generation medications with enhanced efficacy and precision.

四元杂环化合物的合成方法及其生物学意义。
四元杂环合成提供了这些不稳定有机化合物的全面探索,系统地介绍了所有标准四元杂环的合成和反应,同时展示了创造独特变体的各种方法。由于其固有的应变,四元杂环化合物被归类为不稳定的有机化合物,这使得它们作为合成各种复杂杂环分子的前体具有重要的价值。这些化合物已成为药物化学的基本框架,提供独特的性质,加强药物设计和开发。氮、氧、硫等杂原子与四元环(如氮杂啶、氧杂烷、硫杂烷)的结合产生了不同的电子、立体和代谢特征,可以提高治疗效果、选择性和药代动力学。尽管它们的环应变带来了挑战,但化学合成和功能化技术的最新进展使这些化合物更容易用于各种治疗应用。这些张力环结构提供了更高的代谢稳定性,控制亲脂性,以及潜在的有利的结合相互作用,使其适用于多种治疗用途,包括肿瘤,传染病和中枢神经系统疾病。本文综述了四元杂环的主要性质,它们在药物开发中的作用,最近的合成进展,以及这些化合物产生具有更高疗效和精度的下一代药物的潜力。
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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来源期刊
CiteScore
6.40
自引率
2.90%
发文量
186
审稿时长
3-8 weeks
期刊介绍: Current Topics in Medicinal Chemistry is a forum for the review of areas of keen and topical interest to medicinal chemists and others in the allied disciplines. Each issue is solely devoted to a specific topic, containing six to nine reviews, which provide the reader a comprehensive survey of that area. A Guest Editor who is an expert in the topic under review, will assemble each issue. The scope of Current Topics in Medicinal Chemistry will cover all areas of medicinal chemistry, including current developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, compound diversity measurements, drug absorption, drug distribution, metabolism, new and emerging drug targets, natural products, pharmacogenomics, and structure-activity relationships. Medicinal chemistry is a rapidly maturing discipline. The study of how structure and function are related is absolutely essential to understanding the molecular basis of life. Current Topics in Medicinal Chemistry aims to contribute to the growth of scientific knowledge and insight, and facilitate the discovery and development of new therapeutic agents to treat debilitating human disorders. The journal is essential for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important advances.
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