Synthesis and human leukocyte elastase inhibitory evaluation of phosphate triesters and acyl phosphates of penam sulfides and sulfones Original Research Article

The synthesis of 6,6-dibromo-3α-(diphenylphosphate)oxymethyl-2,2-dimethyl penam sulfone (3a), 6α-chloro-3α-(diphenylphosphate)oxymethyl-2,2-dimethyl penam sulfone (3b), benzyl 6α-(diphenyl-phosphate)oxypenicillanate sulfone (4) and 6,6-dibromo-3α-(methylphosphate)carbonyl-2,2-dimethylpenam sulfone (12) are reported. When tested as inhibitors of human leukocyte elastase, the compound 4 proved to be the most active.