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• W2076205184 abstract "Aminopeptidase-catalyzed hydrolysis of Leu-enkephalin and Met-enkephalin is responsible for the rapid metabolism of these pentapeptides in human plasma and at various mucosal sites. The objective of this study was to circumvent this metabolic inactivation by the prodrug approach. A series of 4-imidazolidinone derivatives were prepared by condensing the enkephalins with various aldehydes and ketones and their hydrolysis kinetics were studied in aqueous solution and in the presence of enzymes. Whilst the enkephalins were rapidly hydrolyzed by a purified aminopeptidase and in both human plasma solutions and rabbit intestinal homogenates, the 4-imidazolidinone derivatives were almost totally resistant to enzymatic cleavage in these media. On the other hand, these derivatives are readily converted to the parent peptides by spontaneous hydrolysis. The rate of hydrolysis depended on the structure of the carbonyl component, being apparently increased with increasing steric effects within this component. Thus, the derivative prepared from cyclopentanone showed a half-life of hydrolysis of 3.1 h at pH 7.4 and 37°C whereas the compound made from propionaldehyde had a half-life of 149 h. It is concluded that 4-imidazolidinone formation may be a useful prodrug approach to protect the N-terminal amino acid residue of enkephalins against cleavage by aminopeptidases and to obtain transport forms with improved lipophilicity." @default.
• W2076205184 created "2016-06-24" @default.
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• W2076205184 date "1991-09-01" @default.
• W2076205184 modified "2023-09-24" @default.
• W2076205184 title "Prodrugs of peptides. 15. 4-Imidazolidinone prodrug derivatives of enkephalins to prevent aminopeptidase-catalyzed metabolism in plasma and absorptive mucosae" @default.
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• W2076205184 doi "https://doi.org/10.1016/0378-5173(91)90349-s" @default.
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