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含稳定碳-磷键的裸盖菇素类似物的合成与生物活性

Synthesis and bioactivity of psilocybin analogues containing a stable carbon-phosphorus bond.

作者信息

Vandevelde Marthe, Simoens Andreas, Vandekerckhove Bavo, Stevens Christian

机构信息

Department of Green Chemistry and Technology, Synthesis, Bioresources and Bioorganic Chemistry Research Group, Ghent University Coupure Links 653 9000 Ghent Belgium

出版信息

RSC Med Chem. 2024 Feb 21;15(3):998-1002. doi: 10.1039/d4md00043a. eCollection 2024 Mar 20.

DOI:10.1039/d4md00043a
PMID:38516602
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10953488/
Abstract

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

摘要

已合成了包含不可水解P-C键的裸盖菇素类似物，以评估其生物活性以及对5-羟色胺受体（5-HTR）、5-羟色胺受体（5-HTR）和组织非特异性碱性磷酸酶（TNAP）受体的选择性。未观察到对磷酸酶的活性，然而所有化合物对5-羟色胺受体（5-HTR）和5-羟色胺受体（5-HTR）均表现出良好的结合亲和力，且有一种化合物对5-羟色胺受体（5-HTR）的选择性高于裸盖菇素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/9e79171deabd/d4md00043a-c2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/ec319ba84f62/d4md00043a-c1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/36e4c5ffb679/d4md00043a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/8b5ed1217b2a/d4md00043a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/9e79171deabd/d4md00043a-c2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/ec319ba84f62/d4md00043a-c1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/36e4c5ffb679/d4md00043a-s1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/8b5ed1217b2a/d4md00043a-s2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8cd/10953488/9e79171deabd/d4md00043a-c2.jpg

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本文引用的文献

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Serotonin 2A Receptor (5-HTR) Agonists: Psychedelics and Non-Hallucinogenic Analogues as Emerging Antidepressants.血清素2A受体（5-羟色胺受体）激动剂：作为新型抗抑郁药的致幻剂和非致幻类似物
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Non-hallucinogenic Psychedelic Analog Design: A Promising Direction for Depression Treatment.非致幻性迷幻类似物设计：抑郁症治疗的一个有前景的方向。
Neurosci Bull. 2023 Jan;39(1):170-172. doi: 10.1007/s12264-022-00933-7. Epub 2022 Aug 5.
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Phosphonates and Phosphonate Prodrugs in Medicinal Chemistry: Past Successes and Future Prospects.药物化学中的膦酸盐和膦酸盐前药：过去的成功与未来的前景
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Expert Opin Drug Saf. 2022 Jun;21(6):803-812. doi: 10.1080/14740338.2022.2071422. Epub 2022 May 4.
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