Synthesis and bioactivity of psilocybin analogues containing a stable carbon–phosphorus bond†

IF 3.597 Q2 Pharmacology, Toxicology and Pharmaceutics

MedChemComm Pub Date : 2024-02-21 DOI:10.1039/D4MD00043A

Marthe Vandevelde, Andreas Simoens, Bavo Vandekerckhove and Christian Stevens

引用次数: 0

Abstract

Psilocybin analogues have been synthesized comprising a non-hydrolysable P–C bond to evaluate the biological activity and the selectivity towards 5-HT_2AR, 5-HT_2BR and the TNAP receptor. No activity was observed towards the phosphatase, however all compounds showed good binding affinity for 5-HT_2AR and 5-HT_2BR and one compound showed a higher selectivity towards 5-HT_2AR than psilocin.

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含有稳定碳磷键的迷幻药类似物的合成和生物活性

我们合成了含有不可水解的 P-C 键的迷迭香类似物，以评估其生物活性以及对 5-HT2AR、5-HT2BR 和 TNAP 受体的选择性。没有观察到对磷酸酶的活性，但所有化合物都显示出与 5-HT2AR 和 5-HT2BR 的良好结合亲和力，其中一种化合物对 5-HT2AR 的选择性高于西洛辛。

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

MedChemComm BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL

CiteScore

4.70

自引率

0.00%

发文量

审稿时长

2.2 months

期刊介绍： Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry. In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.