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  • Title: A structure-activity relationship study of spirolactones. Contribution of the cyclopropane ring to antimineralocorticoid activity.
    Author: Chinn LJ, Salamon KW, Desai BN.
    Journal: J Med Chem; 1981 Sep; 24(9):1103-7. PubMed ID: 6270335.
    Abstract:
    A series of spirolactones containing a cyclopropane ring in the molecule was examined for its effects on the mineralocorticoid receptor. The results were compared with those of a similar series of spirolactones in which the cyclopropane ring was replaced by a double bond. Insertion of a double bond or an alpha-cyclopropane ring into the 1,2 or the 6,7 position leads to a reduction in the binding affinity. The pi-bonding system of the beta-cyclopropane ring at C-6 and C-7 does not promote binding to the receptor. The presence of the 6 beta, 7 beta-cyclopropane ring may deter metabolic activation to account for the enhanced in vivo activity.
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