• Archives of Pharmacal Research
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• 제12권2호
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• pp.63-67
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• 1989

The various esters of 20R and 20S-dihydroprednisolonic acid were prepared and evaluated for their local and topical anti-inflammatory activities in rats, including systemic effects. It was demonstrated that the size of the substituent at C-21 and configurational arrangement at C-20 have significant effects on local and topical activity. It was also found that all the derivatives did not show systemic effects as accessed by thymus weight and adrenal weight at the dose level used, while prednisolone showed profound effects on thymus weight.

• Archives of Pharmacal Research
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• 제12권2호
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• pp.68-72
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• 1989

The hydrolysis rates of ester and amide derivatives of 20-dihydroprednisolonic acid were measured in rat serum and liver homogenate. The hydrolysis rate of the esters in serum was found to be faster than that in liver homogenate on the basis of blood volume and liver weight, while the amide derivatives showed much slower change. And it is also found that the size of substituents at C-21 and C-20 configuration expressed considerable effects on the hydrolysis rate of these derivatives.

• Archives of Pharmacal Research
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• 제10권3호
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• pp.184-187
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• 1987

ln order to develope anti-inflammatory glucocorticoids for local use without systemic side-effects, ester and amide derivatives of 20$\xi$-dihydroprednisolonic acid have been prepared. When binding affinities of these compounds to glucocorticoid receptor of rat liver cytosol were compared, all a-isomer at C-20 showed higher binding affinities than the corres¬ponding $\beta$-isomer. The size of the substituents at C-21 had significant influences on binding affinities, which were related with their lipophilicity.