Structure-activity relationship of new steroidal aldosterone antagonists

Wambach, G.; Casals-Stenzel, J.

doi:10.1016/0006-2952(83)90469-0

Cited by 21 publications

(1 citation statement)

References 10 publications

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“…The ability of 18 steroids with structures similar to spironolactone, progesterone or aldosterone to compete with [ 3 H]aldosterone for binding at rat renal cytosol receptors in vitro and the antialdosterone activity in vivo were tested in comparison with spironolactone. The affinity of these compounds for MRs was then compared with their pharmacological action in rats [11].…”

Section: Introductionmentioning

confidence: 99%

Electronic-Topological Study of the Structure-Activity Relationships in a Series of Steroids with Mineralocorticoid Binding Affinity

Kandemi̇rlı

Tokay

Shvets

et al. 2011

Arzneimittelforschung

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Conformational analysis and quantum chemical calculations were carried out using molecular mechanics (MMP2) and semi-empirical quantum chemistry (CNDO/2) methods for 51 steroid homologues belonging to a series of 17-spirolactones. Matrices called Electronic-Topological Matrices of Conjunction (ETMCs) were formed using data obtained from quantum chemical calculations. A structural fragment of activity was identified in the series of steroids. As seen from the fragment's properties, active compounds are characterized by the presence of two atoms of oxygen, O1 and O3, which are situated at a distance of 13.5 A and possess high negative charges (-0.29 to -0.31 e).

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Section: Introductionmentioning

confidence: 99%

Electronic-Topological Study of the Structure-Activity Relationships in a Series of Steroids with Mineralocorticoid Binding Affinity

Kandemi̇rlı

Tokay

Shvets

et al. 2011

Arzneimittelforschung

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Effects of Diuretics on Renal Function

Puschett

Winaver

1992

Comprehensive Physiology

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The sections in this article are: Diuretic Effects on Renal Hemodynamics Drugs That Primarily Alter Glomerular Function Drugs That Primarily Alter Tubular Function Diuretic Effects on Intrarenal Blood Flow Distribution Diuretic Interactions with the Renin–Angiotensin‐Aldosterone system Diuretic Interactions with Prostaglandin Synthesis and with the Inhibition of Prostaglandin Synthetase Nephron Sites of Action and Effects of Diuretics on Solute Excretion Review and Comparison of Methodologies Utility of the Clearance Technique for the Study of Diuretic Site and Mechanism of Action in Man Diuretic Effects on the Excretion of Specific Solutes Cellular and Molecular Actions of Diuretics Carbonic Anhydrase Inhibitors Loop Diuretics Thiazides Mineralcorticoid Antagonists Amiloride

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Steroidal, Aldosterone Antagonists: Increased selectivity of 9α,11‐epoxy derivatives

Grob

Boillaz

Schmidlin

et al. 1997

Helvetica Chimica Acta

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In the search for aldosterone antagonists with an optimal activity profile, twelve 9cc,ll-epoxy-steroids were prepared and compared with their 9a, llcc-unsubstituted analogues in terms of steroid receptor binding in vitro and electrolyte excretion in vivo. Substitution of the parent structures by an epoxy group at positions 9a,ll resulted in marginal effects on mineralocorticoid receptor binding and electrolyte excretion, but greatly reduced androgen and gestagen receptor binding. This finding is reflected in the largely lacking unwanted anti-androgenic and gestagenic side effects in animal models of the three most interesting 9cc,1l-epoxy-spirolactones 4(CGP 33 033), lS(CGP 29245), and 25(CGP 30083).

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Structure-activity relationship of new steroidal aldosterone antagonists

Cited by 21 publications

References 10 publications

Electronic-Topological Study of the Structure-Activity Relationships in a Series of Steroids with Mineralocorticoid Binding Affinity

Electronic-Topological Study of the Structure-Activity Relationships in a Series of Steroids with Mineralocorticoid Binding Affinity

Effects of Diuretics on Renal Function

Steroidal, Aldosterone Antagonists: Increased selectivity of 9α,11‐epoxy derivatives

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