Structure-Activity Relationships of Polyfunctional Diterpenes of the Tigliane Type, V / Preparation and Irritant Activities of Amino Acid and Peptide Esters of Phorbol

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Abstract
Tho synthesis of a series of 12-O-amino acyl- and 12-O-peptidyl-13-acetate and -13,20- diacetate esters of the tetracyclic diterpene alcohol phorbol is described. These esters, which include amino acid moieties with both N-protected and free amino functions, were all tested for irritant activity on mouse ear. The highest activities were observed for esters with N-9-fluorenylmethyloxycarbonyl-protected leucine and 11-aminoundecanoic acid.