Abstract
In order to develope anti-inflammatory glucocorticoids for local use without systemic side-effects, ester and amide derivatives of 20ξ-dihydroprednisolonic acid have been prepared. When binding affinities of these compounds to glucocorticoid receptor of rat liver cytosol were compared, all α-isomer at C-20 showed higher binding affinities than the corresponding β-isomer. The size of the substituents at C-21 had significant influences on binding affinities, which were related with their lipophilicity.
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Kim, H.P., Lee, J.W., Kim, H.J. et al. Development and structural-activity relationship of new local anti-inflammatory steroid, prednisolone derivatives I. Binding affinities to rat liver glucocorticoid receptor. Arch. Pharm. Res. 10, 184–187 (1987). https://doi.org/10.1007/BF02861911
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DOI: https://doi.org/10.1007/BF02861911