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

ABSTRACT: A series of substituted imidazoquinolines, a structurally related chemotype to pyrazoloquinolinones, a well-known class of GABA_A 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.

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Supplementary information

The online version contains supplementary material available at 10.1007/s00706-022-02988-8.

SUBMITTER: Draskovits M 

PROVIDER: S-EPMC10667396 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature