3,8-Disubstituted Pyrazolo[1,5-a]quinazoline as GABA_A Receptor Modulators: Synthesis, Electrophysiological Assays, and Molecular Modelling Studies.

ABSTRACT: As a continuation of our study in the field of GABA_A receptor modulators, we report the design and synthesis of new pyrazolo[1,5-a]quinazoline (PQ) bearing at the 8-position an oxygen or nitrogen function. All the final compounds and some intermediates, showing the three different forms of the pyrazolo[1,5-a]quinazoline scaffold (5-oxo-4,5-dihydro, -4,5-dihydro, and heteroaromatic form), have been screened with an electrophysiological technique on recombinant GABA_AR (α1β2γ2-GABA_AR), expressed in Xenopus laevis oocytes, by evaluating the variation in produced chlorine current, and permitting us to identify some interesting compounds (6d, 8a, 8b, and 14) on which further functional assays were performed. Molecular modelling

SUBMITTER: Crocetti L 

PROVIDER: S-EPMC11477267 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature