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KMID : 0043319870100030184
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Archives of Pharmacal Research
1987 Volume.10 No. 3 p.184 ~ p.187
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Development and Structural-Activity Relationship of New Local Anti-inflammatory Steroid, Prednisolone Derivatives I. Binding Affinities to Rat Liver Glucocorticoid Receptor
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Kim HP
Lee JW/Kim HJ/Byun SM/Lee HJ
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Abstract
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In order to develope anti-inflammatory glucocorticoids for local use without systemic side-effects, ester and amide derivatives of 20xi-dihydroprednisolonic acid have been prepared. When binding affinities of these compounds to glucocorticoid receptor of rat liver cytosol were compared, all alpha-isomer at C-20 showed higher binding affinities than the corresponding beta-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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