Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands

Add time:07/13/2019    Source:sciencedirect.com

The sigma-1 and sigma-2 receptors have been shown to play important roles in CNS diseases, cancer, and other disorders. These findings suggest that targeting these proteins with small-molecule modulators may be of important therapeutic value. Here we report the development of a new class of tetrahydroindazoles that are highly potent and selective ligands for sigma-1. Molecular modeling was used to rationalize the observed structure-activity relationships and identify key interactions responsible for increased potency of the optimized compounds. Assays for solubility and microsomal stability showed this series possesses favorable characteristics and is amenable to further therapeutic development. The compounds described herein will be useful in the development of new chemical probes for sigma-1 and to aid in future work therapeutically targeting this protein.

We also recommend Trading Suppliers and Manufacturers of 2-{[2-(1,3-dioxolan-2-yl)pyridin-1(2H)-yl]methyl}benzenesulfonic acid (cas 3340-21-4). Pls Click Website Link as below: cas 3340-21-4 suppliers

Prev:Synthesis and evaluation of 6-(3-[18F]fluoro-2-hydroxypropyl)-substituted 2-pyridylbenzothiophenes and 2-pyridylbenzothiazoles as potential PET tracers for imaging Aβ plaques
Next:Anti-AIDS agents 86. Synthesis and anti-HIV evaluation of 2′,3′-seco-3′-nor DCP and DCK analogues)