Novel synthetic procedures for C2 substituted imidazoquinolines as ligands for the α/β-interface of the GABAA-receptor.

Autor: Draskovits, Markus, Catorci, Daniele, Wimmer, Laurin, Rehman, Sabah, Siebert, David Chan Bodin, Ernst, Margot, Schnürch, Michael, Mihovilovic, Marko D.
Zdroj: Chemical Monthly / Monatshefte für Chemie; Dec2023, Vol. 154 Issue 12, p1391-1404, 14p
Abstrakt: A series of substituted imidazoquinolines, a structurally related chemotype to pyrazoloquinolinones, a well-known class of GABAA ligands, was prepared via two synthetic procedures and the efficiency of these procedures were compared. One method relies on classical heterocyclic synthesis, the other one aims at late-stage decoration of a truncated scaffold via direct C–H functionalization. A pharmacological evaluation disclosed that one of the synthesized derivatives showed interesting activity on a α1β3 containing receptor subtype. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index