Department of Pharmacy, University of Pisa, Via Bonanno Pisano, 6, 56126 Pisa, Italy.
Department of Pharmacy, University of Naples "Federico II", Via D. Montesano, 49, 80131 Naples, Italy.
Molecules. 2020 May 16;25(10):2331. doi: 10.3390/molecules25102331.
Several indole derivatives have been disclosed by our research groups that have been collaborating for nearly 25 years. The results of our investigations led to a variety of molecules binding selectively to different pharmacological targets, specifically the type A γ-aminobutyric acid (GABA) chloride channel, the translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A adenosine receptor (A AR) and the Kelch-like ECH-associated protein 1 (Keap1). Herein, we describe how these works were conceived and carried out thanks to the versatility of indole nucleus to be exploited in the design and synthesis of drug-like molecules.
我们的研究团队合作近 25 年，已经披露了几种吲哚衍生物。我们的研究结果导致了各种分子选择性地结合到不同的药理靶点，特别是 A 型 γ-氨基丁酸（GABA）氯离子通道、转位蛋白（TSPO）、鼠双微体 2（MDM2）蛋白、A 腺苷受体（A AR）和 Kelch 样 ECH 相关蛋白 1（Keap1）。在这里，我们描述了如何通过吲哚核的多功能性来设计和合成类似药物的分子，从而构思和开展这些工作。
