{"title":"Synthesis and in vitro evaluation of novel amino-phenylmethylene-imidazolone 5-HT2A receptor antagonists†","authors":"Gregory E. Dwulet","doi":"10.1039/D4MD00262H","DOIUrl":null,"url":null,"abstract":"<p >Many drugs target the serotonin 2A (5-HT<small><sub>2A</sub></small>) receptor, including psychedelics, antidepressants, and antipsychotics. This study investigates the 5-HT<small><sub>2A</sub></small> receptor-binding properties of a series of novel compounds with an amino-phenylmethylene-imidazolone (APMI) core structure. Two compounds (<strong>2a</strong> and <strong>2c</strong>) demonstrated significant 5-HT<small><sub>2A</sub></small> 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<small><sub>2A</sub></small> receptor interaction and provides a foundation for developing new 5-HT<small><sub>2A</sub></small> receptor-targeting therapeutic agents.</p>","PeriodicalId":21462,"journal":{"name":"RSC medicinal chemistry","volume":null,"pages":null},"PeriodicalIF":4.1000,"publicationDate":"2024-06-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"RSC medicinal chemistry","FirstCategoryId":"3","ListUrlMain":"https://pubs.rsc.org/en/content/articlelanding/2024/md/d4md00262h","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"BIOCHEMISTRY & MOLECULAR BIOLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Many drugs target the serotonin 2A (5-HT2A) receptor, including psychedelics, antidepressants, and antipsychotics. This study investigates the 5-HT2A 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-HT2A 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-HT2A receptor interaction and provides a foundation for developing new 5-HT2A receptor-targeting therapeutic agents.
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