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Title: Biotransformation studies of di-acid angiotensin converting enzyme inhibitors.
Authors: Drummer, Olaf H;Kourtis, S;Iakovidis, D
Affiliation: University of Melbourne, Department of Medicine Clinical Pharmacology, Austin Hospital, Heidelberg, Victoria, Australia
Issue Date: 1-May-1988
Citation: Arzneimittel-forschung; 38(5): 647-50
Abstract: The biotransformation of di-acid angiotensin converting enzyme inhibitors (I) to cyclized lactam metabolites was studied in the urine of rats using gas chromatography-mass spectrometry. Chemical synthesis of the corresponding piperazine-dione metabolite (III) was achieved by reaction of enalapril, perindopril or ramipril with acetic acid anhydride followed by hydrolysis of the ester group by sodium in ethanol or by acid hydrolysis. Electron impact and chemical ionization mass spectra confirmed the structure of these potential novel metabolites. Selected ion monitoring of urinary extracts demonstrated small amounts (less than 5%) of these lactams for all three inhibitors, however, it was shown that the majority of these lactams were formed as a result of sample treatment rather than due to biotransformation.
Internal ID Number: 3415707
Type: Journal Article
Subjects: Angiotensin-Converting Enzyme Inhibitors.metabolism.urine
Chemical Phenomena
Gas Chromatography-Mass Spectrometry
Indicators and Reagents
Lactams.chemical synthesis.metabolism
Mass Spectrometry
Rats, Inbred Strains
Appears in Collections:Journal articles

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