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The principle of combining a beta-lactam antibiotic with a beta-lactamase inhibitor in a single molecule functioning as pro-drug for the two active components is illustrated by the linked esters 3 and 4 in which ampicillin and mecillinam, respectively, are combined with the beta-lactamase inhibitor penicillanic acid sulfone. It is shown that in man these esters are excellently absorbed from the gastro-intestinal tract and after absorption hydrolyzed with simultaneous liberation of the active components. As a result high blood and tissue levels of antibiotic and beta-lactamase inhibitor in a balanced ratio are attained. The advantages of "mutual pro-drugs" over simple combinations are discussed.
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
June 1996,
International journal of antimicrobial agents,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
June 2005,
Biochemistry,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
August 1986,
Polski tygodnik lekarski (Warsaw, Poland : 1960),
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
April 1986,
Nihon rinsho. Japanese journal of clinical medicine,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
June 2002,
Current medicinal chemistry,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
November 2000,
Antimicrobial agents and chemotherapy,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
January 1989,
The Journal of antimicrobial chemotherapy,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
October 2010,
Expert opinion on therapeutic patents,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
November 1978,
Antimicrobial agents and chemotherapy,
B Baltzer, and
E Binderup, and
W von Daehne, and
W O Godtfredsen, and
K Hansen, and
B Nielsen, and
H Sørensen, and
S Vangedal
March 1984,
Journal of medicinal chemistry,
