SAKAUYE, CAROLYN, AND DAVID FELDMAN. Agonist and antimineralocorticoid activities of spirolactones. Am. J. Physiol. 232(l): 93-97. 1976. -To investigate the mechanism of action of antimineralocorticoids, a series of spirolactone analogues was evaluated for both mineralocorticoid antagonist and agonist activity. Antagonist activity was assessed by inhibition of aldosterone-stimulated sodium tran...

Chiral spirolactones, including spiropropyllactones, spirobutyrolactones, and spirovalerolactones, are important heterocyclic frameworks that attracted the attention of organic medicinal chemists because these motifs constitute core structure several natural products bioactive molecules. The absolute configuration substituents on fully substituted spirocyclic stereocenter lactone can potentiall...

Spirolactones are potent antagonists of the mineralocorticoid receptor (MR), a ligand-induced transcription factor belonging to the nuclear receptor superfamily. Spirolactones are synthetic molecules characterized by the presence of a C17 gamma-lactone, which is responsible for their antagonist character. They harbor various substituents at several positions of the steroid skeleton that modulat...

The aim of this work was the design, synthesis, and characterization new chromogenic spirolactone dyes based on a 2-phenyl-1-benzopyrylium (flavylium) backbone for further development thermochromic smart labels. influence electron-donating electron-withdrawing groups five synthesized studied in terms color modification, acid-base behavior properties. By using UV–Vis absorption emission spectros...

An unusual C18 norditerpenoid, aspergiloid I (1), was isolated from the culture broth of Aspergillus sp. YXf3, an endophytic fungus derived from Ginkgo biloba. Its structure was unambiguously established by analysis of HRMS-ESI and spectroscopic data, and the absolute configuration was determined by low-temperature (100 K) single crystal X-ray diffraction with Cu Kα radiation. This compound is ...

Hydroxylated rhodamines, carbopyronines, silico- and germanorhodamines with absorption maxima in the range of 530-640 nm were prepared and applied in specific labeling of living cells. The direct and high-yielding entry to germa- and silaxanthones tolerates the presence of protected heteroatoms and may be considered for the syntheses of various sila- and germafluoresceins, as well as -rhodols. ...

The heterogeneity of the lysine-rich histone from several mammalian cells has been studied. The molecules were cleaved with N-bromosuccinimide and separated into three fractions by exclusion chromatography. The three fractions were Fraction 1, the NHz-terminal peptide of molecular weight -6000 which proved to be highly heterogeneous upon electrophoretic analysis; Fraction 2, the COOH-terminal f...

A heme d prosthetic group with the configuration of a cis-hydroxychlorin gamma-spirolactone has been found in the crystal structures of Penicillium vitale catalase and Escherichia coli catalase hydroperoxidase II (HPII). The absolute stereochemistry of the two heme d chiral carbon atoms has been shown to be identical. For both catalases the heme d is rotated 180 degrees about the axis defined b...