INVESTIGADORES
BOSCHETTI Carlos Eugenio
artículos
Título:
Synthesis and Elastase Inhibitory Activity of 6 -Chloro-2,2-Dimethyl-3 -(Pivaloyloxy)methylpenam Sulfone, 6 -Chloro-2,2-Dimethyl-3-exo-Methylene penam Sulfone, Benzyl and Methyl 6 -Substituted Penicillanate Sulfones
Autor/es:
CARLOS EUGENIO BOSCHETTI; ORESTE MASCARETTI,; JULIA CRICCO,; OSCAR ROVERI,
Revista:
BIOORGANIC & MEDICINAL CHEMISTRY.
Editorial:
PERGAMON-ELSEVIER SCIENCE LTD
Referencias:
Año: 1995 vol. 3 p. 95 - 100
ISSN:
0968-0896
Resumen:
The triflates and pivalates of 3ct-hydroxymethyl-6-substituted-2,2-dimethylpenam sulfones 3, 5; methyl and benzyl 6-substituted penicillanates 6--9 and 3-exo-methylene-6-substituted-2,2-dimethylpenam sulfone 4 were synthesized. These novelcompounds were evaluated as elastase inhibitors using porcine pancreatic elastase. The effects that structural modifications ofsubstituents on C-3 and C-6 in the penam nucleus have on elastase activity were examined and several similarities anddistinctions were identified when compared to the reported penicillin esters and amides elastase inhibitors.