benzofurans has been researched along with pyrroline* in 1 studies
1 other study(ies) available for benzofurans and pyrroline
Article | Year |
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Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.
Dihydrofuran-2-one and dihydropyrrol-2-one derivatives were identified as novel, potent and selective mineralocorticoid receptor (MR) antagonists by the structure-based drug design approach utilizing the crystal structure of MR/compound complex. Introduction of lipophilic substituents directed toward the unfilled spaces of the MR and identification of a new scaffold, dihydropyrrol-2-one ring, led to potent in vitro activity. Among the synthesized compounds, dihydropyrrol-2-one 11i showed an excellent in vitro activity (MR binding IC50=43nM) and high selectivity over closely related steroid receptors such as the androgen receptor (AR), progesterone receptor (PR) and glucocorticoid receptor (GR) (>200-fold for AR and PR, 100-fold for GR). Topics: Animals; Benzofurans; Benzoxazines; Chlorocebus aethiops; COS Cells; Crystallography, X-Ray; Drug Design; Inhibitory Concentration 50; Mineralocorticoid Receptor Antagonists; Protein Binding; Pyrroles; Structure-Activity Relationship | 2013 |