Institute of Pharmaceutical Chemistry, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Institute of Pharmaceutical Chemistry, Interdisciplinary Excellence Center, University of Szeged, H-6720 Szeged, Hungary.
Int J Mol Sci. 2021 Nov 3;22(21):11935. doi: 10.3390/ijms222111935.
Kynurenic acid (KYNA) is an endogenous neuroprotective agent of increasing importance. Several derivatives have already been synthesized, bearing an abundance of functional groups attached to the main skeleton in different positions. Several of these compounds have already been tested in biological evaluations, with several of them targeting the same receptors and biological effects as KYNA. However, these modified compounds build upon the unmodified KYNA skeleton leaving a possible route for the synthesis of new, potentially neuroprotective derivatives with heteroatom-containing ring systems. The aim of this review is to summarize the syntheses of KYNA derivatives with altered skeletons and to pinpoint an appealing transformation for future medicinal lead molecules.
犬尿酸（KYNA）是一种内源性神经保护剂，其重要性日益增加。已经合成了几种衍生物，它们在主骨架上的不同位置带有丰富的官能团。其中一些化合物已经在生物评价中进行了测试，其中一些化合物的作用靶点和生物学效应与 KYNA 相同。然而，这些修饰化合物是在未修饰的 KYNA 骨架的基础上构建的，为合成具有杂原子含环系统的新型潜在神经保护衍生物提供了可能的途径。本文综述了改变骨架的 KYNA 衍生物的合成方法，并指出了一种有吸引力的转化方法，有望成为未来的药用先导分子。
