) "Synthesis and human leukocyte elastase inhibitory evaluation of phosphate triesters and acyl phosphates of penam sulfides and sulfones".

LABORDE, M; PEZZENATI, G; MASCARETTI, O.; ROSSI, R.C.; ROSSI, J.P.F.C

BIOORGANIC & MEDICINAL CHEMISTRY.

Elsevier

Lugar: London; Año: 2001 p. 2113 - 2117

0968-0896

Abstract—The synthesis of 6,6-dibromo-3a-(diphenylphosphate)oxymethyl-2,2-dimethyl penam sulfone (3a), 6a-chloro-3a-(diphenylphosphate)oxymethyl-2,2-dimethyl penam sulfone (3b), benzyl 6a-(diphenyl-phosphate)oxypenicillanate sulfone (4) and 6,6-dibromo-3a-(methylphosphate)carbonyl-2,2-dimethylpenam sulfone (12) are reported. When tested as inhibitors of human leukocyteelastase, the compound 4 proved to be the most active. # 2001Elsevier Science Ltd. All rights reserved.