Abstract：
:We have investigated the in vitro metabolism of three small antimicrobial β(2,2)-amino acid derivatives (M (w) < 500) that are highly potent against methicillin resistant Staphylococcus aureus, and are among the first compounds designed from small cationic antimicrobial peptides with potential for oral administration. The β(2,2)-amino acid derivatives are virtually completely resistant against degradation by proteases, and to further explore their drug potential, we have investigated the hepatic Phase I metabolism of this class of antimicrobial compounds. The β(2,2)-amino acid derivatives were incubated with murine liver microsomes and the metabolites analyzed semi-quantitatively by HPLC-MS and qualitatively by ultra performance liquid chromatography coupled to a tandem mass spectrometer which enabled identification of the metabolites by careful interpretation of the collision activated dissociation spectra. The study shows that sterically hindered β(2,2)-amino acid derivatives that otherwise are stable against proteolytic degradation underwent Phase I metabolism and were oxidized to a number of different metabolites depending on the structure of the β(2,2)-amino acid side-chains.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Hansen T,Moe MK,Anderssen T,Strøm MBdoi
10.1007/s13318-012-0086-9subject
Has Abstractpub_date
2012-09-01 00:00:00pages
191-201issue
3eissn
0378-7966issn
2107-0180journal_volume
37pub_type
杂志文章abstract：:The disposition kinetics of the N-oxide of picobenzide were studied after administration to rabbits at a bolus dose of 30 mg/kg of picobenzide intravenously. The biotransformation process fits a first-order kinetic process, and the metabolite shows good access capacity to the peripheral compartment. The N-oxide of pic...
journal_title：European journal of drug metabolism and pharmacokinetics
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更新日期：1989-01-01 00:00:00
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
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abstract：:COR3224 is a new 2-amino-2 oxazoline derivative with antidepressant properties. The distribution, excretion and metabolism of radiochemically labelled 14C-COR3224 has been investigated in the rat after intravenous injection. The compound was widely distributed and rapidly excreted. Hydroxylation and sulphate conjugati...
journal_title：European journal of drug metabolism and pharmacokinetics
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doi：
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更新日期：2016-08-01 00:00:00
abstract：:The present study was carried out to find the in vivo performance of guar gum-based colon-targeted tablets of metronidazole as compared to an immediate release tablets in human volunteers. Six healthy volunteers participated in the study and a crossover design was used. Blood samples were obtained at different time in...
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journal_title：European journal of drug metabolism and pharmacokinetics
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journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
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