Grzegorz Satała

TL;DR: A series of new quinoline- and isoquinoline-sulfonamide analogs of aripiprazole was synthesized to explore the influence of two structural features - replacement of ether/amide moiety with sulfonamide one, and localization of a sulf onamide group in the azine moiety.

TL;DR: Two series of arylpiperazinyl-alkyl quinoline-, isoquinoline-, naphthalene-sulfonamides with flexible and semi-rigid alkylene spacer produced antidepressant-like effects in the forced swim test in mice and showed significant anxiolytic activity in the plus-maze test in rats.

TL;DR: The design, synthesis, and characterization of a novel class of 5-HT6R antagonists that is based on the 1H-pyrrolo[3,2-c]quinoline core are reported, and results are promising enough to warrant further detailed mechanistic studies on the therapeutic potential of5-HT 6R antagonists and inverse agonists for the treatment of cognitive decline and depression/anxiety symptoms that are comorbidities of Alzheimer's disease.

TL;DR: A series of new derivatives of N‐(2‐methoxyphenyl)piperazine have been synthesized for their affinity toward serotonergic receptors and for their potential antidepressant‐like activity, with the most promising compound exhibiting affinity toward receptors Ki <1 nm (5‐HT1A) and Ki = 34 nm ( 5‐HT7).

TL;DR: Taking into account the beneficial properties of 13, i.e., good drug‐like parameters, the significant antagonistic action, high selectivity to 5‐HT7R, and its in vivo antidepressant‐like activity, the compound should be considered as a new lead in the search for drugs acting on CNS via 5‐ HT7 receptor.