benzofurans and pyrroline

benzofurans has been researched along with pyrroline* in 1 studies

Other Studies

1 other study(ies) available for benzofurans and pyrroline

Article	Year
Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists. Bioorganic & medicinal chemistry, 2013, Oct-01, Volume: 21, Issue:19 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

Article

Year

Design, synthesis, and structure-activity relationships of dihydrofuran-2-one and dihydropyrrol-2-one derivatives as novel benzoxazin-3-one-based mineralocorticoid receptor antagonists.

Bioorganic & medicinal chemistry, 2013, Oct-01, Volume: 21, Issue:19

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