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Stability of meropenem and effect of 1 beta-methyl substitution on its stability in the presence of renal dehydropeptidase I
Author(s) -
MASATOMO FUKASAWA,
Yoshihiro Sumita,
E.T. Harabe,
Tomoharu Tanio,
HIROSHI NOUDA,
Tsuneo Kohzuki,
T. OKUDA,
Hideaki Matsumura,
Masataka Sunagawa
Publication year - 1992
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.36.7.1577
Subject(s) - meropenem , imipenem , chemistry , antibacterial agent , pharmacology , antibiotics , biology , stereochemistry , biochemistry , antibiotic resistance
The stability of meropenem in the presence of renal dehydropeptidase I (DHP-I) varied extremely with the animal source of the enzyme. Meropenem, compared with imipenem, was rather easily hydrolyzed by DHP-Is from mice, rabbits, and monkeys, while it showed a higher resistance to guinea pig and beagle dog DHP-Is. In addition, meropenem was four times more resistant than imipenem to human DHP-I. The 1 beta-methyl substituent on carbapenems, i.e., meropenem and 1 beta-methyl imipenem, made them considerably more resistant to mouse and swine DHP-Is than the 1-unsubstituted derivatives are.

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