Beta-lactamase inhibitor prodrug

作者: Dale Gordon Pfizer Global Res. Dev. Mcleod , Anthony Pfizer Global Res. Dev. Marfat

DOI:

关键词: Beta-lactamaseAntibioticsPharmacologyChemistryTherapeutic effectivenessProdrugSulfone

摘要: Prodrugs of 6-s-hydroxymethylpenicillanic acid sulfone having the structure wherein R is H or methyl, and solvates thereof, are disclosed. Also disclosed pharmaceutical compositions comprising a prodrug present invention, solvate an optional beta-lactam antibiotic at least one pharmaceutically acceptable carrier. Further method for increasing therapeutic effectiveness in mammal by administering effective amount betalactam effectiveness-increasing thereof. Additionally treating bacterial infection therapeutically composition invention to need

参考文章(23)
I. Jacob Pachter, Maxwell Gordon, Method for treating resistant bacteria including anaerobes ,(1981)
Olof Harald Sjoberg, Bertil Ake Ekstrom, Odon Kalman Jozsef Kovacs, New penicillin esters and methods and compositions for treating infectious diseases ,(1973)
Alfredo Cugola, Giovanni Gaviraghi, Indole derivatives and pharmaceutical use thereof ,(1993)
Robert Fischer Myers, Penicillanic acid dioxide prodrug ,(1982)
Venkata Ramana Doppalapudi, Akireddy Srinivasa Rao, John D. Buynak, Penicillanic acid derivative compounds and methods of making ,(2004)
Arthur R. English, Dennis Girard, V. John Jasys, Robert J. Martingano, Michael S. Kellogg, Orally effective acid prodrugs of the beta-lactamase inhibitor sulbactam. Journal of Medicinal Chemistry. ,vol. 33, pp. 344- 347 ,(1990) , 10.1021/JM00163A055