Di Fabio, Romano; Arban, Roberto; Bernasconi, Giovanni; Braggio, Simone; Blaney, Frank E.; Capelli, Anna M.; Castiglioni, Emiliano; Donati, Daniele; Fazzolari, Elettra; Ratti, Emiliangelo; Feriani, Aldo; Contini, Stefania; Gentile, Gabriella; Ghirlanda, Damiano; Sabbatini, Fabio M.; Andreotti, Daniele; Spada, Simone; Marchioro, Carla; Worby, Angela; St-Denis, Yves published the artcile< Dihydropyrrole[2,3-d]pyridine Derivatives as Novel Corticotropin-Releasing Factor-1 Antagonists: Mapping of the Receptor Binding Pocket by in Silico Docking Studies>, COA of Formula: C9H9Cl2NO2, the main research area is pyrrolo pyridine preparation CRF1 antagonist antidepressant SAR.
In an effort to discover novel CRF-1 receptor antagonists exhibiting improved physicochem. properties, a dihydropirrole[2,3]pyridine scaffold was designed and explored in terms of the SAR of the substitution at the pendent Ph ring and the nature of the heterocyclic moieties present in the upper region of the mol. Selective and potent compounds have been discovered endowed with reduced ClogP with respect to compounds known in the literature. Of particular relevance was the finding that the in vitro affinity of the series was maintained by reducing the overall lipophilicity. The results achieved by this exploration enabled the formulation of a novel hypothesis on the nature of the receptor binding pocket of this class of CRF-1 receptor antagonists, making use of in silico docking studies of the putative nonpeptidic antagonist binding site set up in house by homol. modeling techniques.
Journal of Medicinal Chemistry published new progress about Antidepressants. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, COA of Formula: C9H9Cl2NO2.