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

Marthe Vandevelde Andreas Simoens Bavo Vandekerckhove Christian V Stevens

Published in: RSC medicinal chemistry (2024)

Psilocybin analogues have been synthesized comprising a non-hydrolysable P-C bond to evaluate the biological activity and the selectivity towards 5-HT 2A R, 5-HT 2B R and the TNAP receptor. No activity was observed towards the phosphatase, however all compounds showed good binding affinity for 5-HT 2A R and 5-HT 2B R and one compound showed a higher selectivity towards 5-HT 2A R than psilocin.

Keyphrases

molecular docking
binding protein
risk assessment
mass spectrometry
heavy metals
structural basis
transition metal