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

Authors
Laborde, M Pezzenati, G Yovaldi, P Mascaretti, OA Rossi, RC Rossi, JP
Citation
M. Laborde et al., Synthesis and human leukocyte elastase inhibitory evaluation of phosphate triesters and acyl phosphates of penam sulfides and sulfones, BIO MED CH, 9(8), 2001, pp. 2113-2117
Citations number
38
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
9
Issue
8
Year of publication
2001
Pages
2113 - 2117
Database
ISI
SICI code
0968-0896(200108)9:8<2113:SAHLEI>2.0.ZU;2-Y
Abstract
The synthesis of 6,6-dibromo-3 alpha-(diphenylphosphate)oxymethyl-2,2-dimet hyl penam sulfone (3a), 6 alpha -chloro-3 alpha-(diphenylphosphate)oxymethy l-2,2-dimethyl penam sulfone (3b), benzyl 6 alpha-(diphenyl-phosphate)oxype nicillanate sulfone (4) and 6,6-dibromo-3 alpha-(methylphosphate)carbonyl-2 ,2-dimethylpenam sulfone (12) are reported. When tested as inhibitors of hu man leukocyte elastase, the compound 4 proved to be the most active. (C) 20 01 Elsevier Science Ltd. All rights reserved.