Abstract
N G-Acylated argininamides, covering a broad range of lipophilicity (calculated log D values: −1.8–12.5), were synthesized and investigated for NPY Y 1 receptor (Y 1R) antagonism, Y 1R affinity and stability in buffer ( N G-deacylation, yielding BIBP 3226). Broad structural variation of substituents was tolerated. The K i (binding) and K b values (Y 1R antagonism) varied from low nM to one-digit μM. Most of the compounds proved to be sufficiently stable at pH 7.4 over 90 min to determine reliable pharmacological data in vitro. Exceptionally high instability was detected when a succinyl moiety was attached to the guanidine, probably, due to an intramolecular cleavage mechanism.
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