Ontology highlight
ABSTRACT:
SUBMITTER: Hogendorf AS
PROVIDER: S-EPMC5431432 | biostudies-literature | 2017 May
REPOSITORIES: biostudies-literature
Hogendorf Adam S AS Hogendorf Agata A Kurczab Rafał R Satała Grzegorz G Lenda Tomasz T Walczak Maria M Latacz Gniewomir G Handzlik Jadwiga J Kieć-Kononowicz Katarzyna K Wierońska Joanna M JM Woźniak Monika M Cieślik Paulina P Bugno Ryszard R Staroń Jakub J Bojarski Andrzej J AJ
Scientific reports 20170504 1
A series of 5-aryl-1-alkylimidazole derivatives was synthesized using the van Leusen multicomponent reaction. The chemotype is the first example of low-basicity scaffolds exhibiting high affinity for 5-HT<sub>7</sub> receptor together with agonist function. The chosen lead compounds 3-(1-ethyl-1H-imidazol-5-yl)-5-iodo-1H-indole (AGH-107, 1o, K <sub>i 5-HT7</sub> = 6 nM, EC<sub>50</sub> = 19 nM, 176-fold selectivity over 5-HT<sub>1A</sub>R) and 1e (5-methoxy analogue, K <sub>i 5-HT7</sub> = 30 nM ...[more]