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Titolo:
ON THE REACTIONS OF THE CARBAPENEM, MEROPENEM, IN THE SOLUBLE FRACTION OF RAT-KIDNEY
Autore:
ROY AB; HEWLINS MJE;
Indirizzi:
UNIV WALES COLL CARDIFF,COLL CARDIFF,DEPT BIOCHEM CARDIFF CF1 1ST WALES UNIV WALES COLL CARDIFF,COLL CARDIFF,SCH CHEM & APPL CHEM CARDIFF CF11ST WALES
Titolo Testata:
Xenobiotica
fascicolo: 3, volume: 24, anno: 1994,
pagine: 185 - 198
SICI:
0049-8254(1994)24:3<185:OTROTC>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
BETA-LACTAMASE ACTIVITY; DEHYDROPEPTIDASE-I; RENAL DIPEPTIDASE; THIENAMYCIN; HYDROLYSIS; IMIPENEM; ENZYMES; CYSTEINYLGLYCINE; GLUTATHIONE; DERIVATIVES;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
A.B. Roy e M.J.E. Hewlins, "ON THE REACTIONS OF THE CARBAPENEM, MEROPENEM, IN THE SOLUBLE FRACTION OF RAT-KIDNEY", Xenobiotica, 24(3), 1994, pp. 185-198

Abstract

1. When meropenem (I) is incubated with the soluble fraction of rat kidney or its ultrafiltrate the carbapenem disappears at a rate of 50 nmol/min per g of kidney at pH 8.4 and 37-degrees-C. 2. In both cases the kinetics are inconsistent with the reaction being enzymic and the product has been shown to be a thiol. 3. The same reaction occurs in similar preparations from the kidney of several other mammalian species.4. The reaction of meropenem with thiols has been investigated: only those having a vicinal amino group react rapidly. 5. The product of the reaction with cysteine has been characterized as the amide (III) of the latter with meropenoic acid (II), the carboxylic acid formed by the hydrolysis of the beta-lactam ring of meropenem. 6. It is postulatedthat the destruction of meropenem in the soluble fraction of rat kidney occurs by the non-enzymic reaction of the carbapenem with endogenous cysteine or related thiols. 7. There is no evidence that this reaction can occur in vivo but it should be considered in the future design of carbapenems.

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Documento generato il 30/11/20 alle ore 00:43:14