Development of tetrahydroindazole-based potent and selective sigma-2 receptor ligands.

Development of tetrahydroindazole-based potent and selective sigma-2 receptor ligands. ChemMedChem. 2019 May 09;: Authors: Iyamu ID, Lv W, Malik N, Mishra RK, Schiltz GE Abstract The sigma-2 receptor has been shown to play important roles in a number of important diseases, including CNS disorders and cancer. However, mechanisms by which sigma-2 contributes to these diseases remain unclear. Development of new sigma-2 ligands that can be used to probe the function of this protein and potentially as drug discovery leads are therefore of great importance. Here we report the development of a series of tetrahydroindazole compounds that are highly potent and selective for sigma-2. The structure-activity relationship data was used to generate a pharmacophore model which summarizes the common features present in the potent ligands. Assays for solubility and microsomal stability showed that several members of this compound series possessed promising characteristics for further development of useful chemical probes or drug discovery leads. PMID: 31071238 [PubMed - as supplied by publisher]
Source: ChemMedChem - Category: Chemistry Authors: Tags: ChemMedChem Source Type: research