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Synthesis of a Thiol Building Block for the Crystallization of a Semiconducting Gyroidal Metal-sulfur Framework
Published on: April 9, 2018
6-Sulfonylbenzothiazolones as potential scaffolds for the design of 5-HT6 ligands
Paul-Emmanuel Larchanche1, Vincent Ultré2, Delphine Le Broc3
1Université de Lille, F-59000 Lille, France; UDSL, EA 4481, UFR Pharmacie, F-59000 Lille, France; Inserm UMR-S1172, Jean-Pierre Aubert Research Center, F-59000 Lille, France.
Abstract:
5-HT6 Receptors are relatively recently discovered receptors that interact with cholinergic, glutamatergic, GABAergic and dopaminergic transmission systems. These receptors have been implicated in the CNS system as therapeutic targets in applications such as psychosis, reduction of body weight or Alzheimer's disease. As part of our efforts to develop 5-HT6 antagonists, we explored the benzothiazolone scaffold substituted in position 3 or 6 respectively with ethylamino chains and an aromatic ring connected through a sulfonyl linker. Final compounds were evaluated in radioligand binding assays for their ability to interact with 5-HT6 receptors. Their potential cytotoxic effects were determined on the human neuroblastoma cell line SY5Y. They showed very low cytotoxicity, and one of them has submicromolar affinity for 5-HT6 receptors.
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