Synthesis and Local Anti-inflammatory Activity of Esters of 20R- and 20S-Dihydroprednisolonic Acid

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.