Development and structural-activity relationship of new local anti-inflammatory steroid, prednisolone derivatives I. Binding affinities to rat liver glucocorticoid receptor

초록

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. © 1987 The Pharmaceutical Society of Korea.

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