Agnieszka Zagórska, Anna Partyka, Magdalena Jastrzębska-Więsek, Anna Czopek, Monika Fryc, Agata Siwek, Monika Głuch-Lutwin, Barbara Mordyl, Anna Maślanka, Anna Jaromin, Rafał Kurczab
The new dual 5HT1A /5HT7 receptor ligands were designed based on the purine-2,6-dione scaffold with the fluorine atom. Twenty-one new derivatives were synthesized, and their structure-activity relationship was summarized. Compound 11 (7-(2-(3-fluorophenyl)-2-oxoethyl)-8-((4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)amino)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione) showed the highest affinity to 5HT1A R and 5HT7 R, and was the most potent antagonist of 5-HT1A R (Kb = 0.26 ± 0.1 nM) which activity can be to reference compound NAN-190 (Kb = 0...
July 19, 2023: Bioorganic Chemistry