ISSN:
1573-3904
Keywords:
Cholecystokinin
;
N-(2-carboxyethyl)amines
;
CDMT
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
Notes:
Summary The involvement of cholecystokinin receptors in the phenomenon of satiety has been the impetus for significant research efforts, leading to the design and synthesis of CCK-A selective agonists for the possible treatment of obesity. The Abbott laboratories have described a novel series of pseudotetrapeptides represented by compound A71623, a highly potent and selective peripheral receptor agonist, but possessing very poor bioavailability. Starting from the structural requirements of this series of compounds, a peptidomimetic study was investigated, especially focusing on the N-terminal part of A71623. Using standard coupling methods, introduction of unnatural aromatic amino acids bearing a 2-carboxyethyl side chain on their α-amino group, along with backbone length modulation, afforded selective analogues, presenting a highly modified peptidic backbone. From our two lead compounds, further optimization is under development, tending towards nonpeptidic structures.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF02442882
Permalink
