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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.
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
January 2003,
Chirality,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
July 1948,
Journal of the American Chemical Society,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
January 2009,
Bioorganic & medicinal chemistry letters,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
July 2006,
Bioorganic & medicinal chemistry letters,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
March 2014,
Organic letters,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
January 2009,
Bioorganic & medicinal chemistry letters,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
January 2010,
Amino acids,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
June 2018,
Chirality,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
December 2011,
Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine,
A Leone-Bay, and
N Santiago, and
D Achan, and
K Chaudhary, and
F DeMorin, and
L Falzarano, and
S Haas, and
S Kalbag, and
D Kaplan, and
H Leipold
May 2004,
The Journal of organic chemistry,
