Design, Synthesis and Biological Evaluation of Novel 1,3,5-Triazines: Effect of Aromatic Ring Decoration on Affinity to 5-HT₇ Receptor.

ABSTRACT: Considering the key functions of the 5-HT₇ receptor, especially in psychiatry, and the fact that effective and selective 5-HT₇ receptor ligands are yet to be available, in this work, we designed and synthesized novel 1,3,5-triazine derivatives particularly based on the evaluation of the effect of substituents at aromatic rings on biological activity. The tested compounds showed high affinity to the 5-HT₇ receptor, particularly ligands N²-(2-(5-fluoro-1H-indol-3-yl)ethyl)-N⁴-phenethyl-1,3,5-triazine-2,4,6-triamine 2 (K_i = 8 nM) and N²-(2-(1H-indol-3-yl)ethyl)-N⁴-(2-((4-fluorophenyl)amino)ethyl)-1,3,5-triazine-2,4,6-triamine 12 (K_i = 18 nM) which showed moderate meta

SUBMITTER: Kulaga D 

PROVIDER: S-EPMC9656787 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature