| Literature DB >> 7473553 |
A Leone-Bay1, N Santiago, D Achan, K Chaudhary, F DeMorin, L Falzarano, S Haas, S Kalbag, D Kaplan, H Leipold.
Abstract
A series of N-acylated alpha-amino acids were synthesized and shown to improve the oral delivery of two protein drugs, salmon calcitonin (sCT) and interferon-alpha. Forty-five compounds in this series were tested in vivo in rats and primates. A significant positive correlation was found between the log P of the acylated amino acids and the decrease in serum calcium following oral dosage of sCT in rats. Such a correlation was not found for interferon-alpha. These derivatized amino acids only weakly inhibited the activity of trypsin or leucine aminopeptidase. Histological examinations of rat intestinal tissue after oral dosing of acylated amino acid/protein combinations revealed no detectable pathology.Entities:
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Year: 1995 PMID： 7473553 DOI： 10.1021/jm00021a015
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446