Morpholine is a heterocycle featured in numerous approved and experimental drugs as well as bioactive molecules. It is often employed in the field of medicinal chemistry for its advantageous physicochemical, biological, and metabolic properties, as well as its facile synthetic routes. The morpholine ring is a versatile and readily accessible synthetic building block, it is easily introduced as an amine reagent or can be built according to a variety of available synthetic methodologies. This versatile scaffold, appropriately substituted, possesses a wide range of biological activities. There are many examples of molecular targets of morpholine bioactive in which the significant contribution of the morpholine moiety has been demonstrated; it is an integral component of the pharmacophore for certain enzyme active‐site inhibitors whereas it bestows selective affinity for a wide range of receptors. A large body of in vivo studies has demonstrated morpholine's potential to not only increase potency but also provide compounds with desirable drug‐like properties and improved pharamacokinetics. In this review we describe the medicinal chemistry/pharmacological activity of morpholine derivatives on various therapeutically related molecular targets, attempting to highlight the importance of the morpholine ring in drug design and development as well as to justify its classification as a privileged structure.

中文翻译：

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吗啉作为一种特权结构：含有吗啉的生物活性分子的药物化学和药理活性综述。

吗啉是许多批准和实验药物以及生物活性分子中的杂环。它以其优越的物理化学，生物学和代谢特性以及便捷的合成路线而经常用于药物化学领域。吗啉环是一种通用且易于使用的合成构件，可以轻松地作为胺试剂引入，也可以根据多种可用的合成方法进行构建。这种多用途的支架，经过适当的替换，具有广泛的生物学活性。有许多示例性的吗啉生物活性分子靶标，其中已经证明了吗啉部分的重要作用。它是某些酶活性部位抑制剂的药效基团不可或缺的组成部分，同时赋予了广泛的受体选择性亲和力。大量的体内研究表明吗啉不仅具有增强药效的潜力，而且还可以提供具有理想的类药物特性和改善的药代动力学的化合物。在这篇综述中，我们描述了吗啉衍生物对各种治疗相关分子靶标的药用化学/药理活性，试图强调吗啉环在药物设计和开发中的重要性，并证明其作为特权结构的合理性。不仅可以提高药效，而且还可以提供具有理想的类药物特性和改善的药代动力学的化合物。在这篇综述中，我们描述了吗啉衍生物对各种治疗相关分子靶标的药用化学/药理活性，试图强调吗啉环在药物设计和开发中的重要性，并证明其作为特权结构的合理性。不仅可以提高药效，而且还可以提供具有理想的类药物特性和改善的药代动力学的化合物。在这篇综述中，我们描述了吗啉衍生物对各种治疗相关分子靶标的药用化学/药理活性，试图强调吗啉环在药物设计和开发中的重要性，并证明其作为特权结构的合理性。