Synthesis and in vitro evaluation of novel amino-phenylmethylene-imidazolone 5-HT 2A receptor antagonists.

Autor: Dwulet GE; Independent Researcher Bellingham Washington USA gedwulet@pm.me.
Jazyk: angličtina
Zdroj: RSC medicinal chemistry [RSC Med Chem] 2024 Jun 14; Vol. 15 (7), pp. 2508-2513. Date of Electronic Publication: 2024 Jun 14 (Print Publication: 2024).
DOI: 10.1039/d4md00262h
Abstrakt: Many drugs target the serotonin 2A (5-HT 2A ) receptor, including psychedelics, antidepressants, and antipsychotics. This study investigates the 5-HT 2A receptor-binding properties of a series of novel compounds with an amino-phenylmethylene-imidazolone (APMI) core structure. Two compounds (2a and 2c) demonstrated significant 5-HT 2A receptor-binding affinity without agonistic activity, instead displaying antagonistic effects. Structurally, these compounds differ from previously reported phenethylamine-based antagonists. This work introduces APMIs as a novel pharmacophore for 5-HT 2A receptor interaction and provides a foundation for developing new 5-HT 2A receptor-targeting therapeutic agents.
Competing Interests: There is no conflict of interest to declare.
(This journal is © The Royal Society of Chemistry.)
Databáze: MEDLINE
Externí odkaz: