The Importance of Stereochemistry in 5-HT₇R Modulation─A Case Study of Hydantoin Derivatives.

ABSTRACT: Serotonin 5-HT₇ receptor (5-HT₇R), one of the most recently discovered members of the serotonergic system, has become a promising target in the search for central nervous system disorders. Despite the number of preclinical results, none of the selective 5-HT₇R agents has been approved; therefore, the clinical significance of this protein has not been confirmed yet. Recently, we described very promising, selective, and highly potent hydantoin-derived 5-HT₇R antagonists with confirmed antidepressant activity in vivo and a very good ADMET profile; however, they have been tested in behavioral studies as racemates. In this work, the synthesis of optically pure hydantoin-derived 5-HT₇R agents using cost-effective, classical methods ha

SUBMITTER: Kucwaj-Brysz K 

PROVIDER: S-EPMC11587507 | biostudies-literature | 2024 Nov

REPOSITORIES: biostudies-literature