Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives

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Abstract
Several steroid derivatives having .DELTA.11-pregnane skeleton with a 17-.gamma.-spirolactone function were synthesized to evaluate their antialdosterone activity and to elucidate the relation between their binding affinity to mineralocorticoid receptor (MR) and their mineralo- and/or antimineralocorticoid activity. Although many of the synthesized compounds showed strong binding affinity for the MR and aldosterone agonist activity, 3-(17.beta.-hydroxy-3-oxoandrosta-1,4,6,11-tetraen-17.alpha.-yl)propionic acid .gamma.-lactone (12) exhibited good aldosterone antagonist activity in an in vivo assay [rat]. Its in vivo antiandrogenic activity was also found to be relatively weak.