Weiss, Stefan and Keller, Max and Bernhardt, Guenther and Buschauer, Armin and Koenig, Burkhard (2010) N-G-Acyl-argininamides as NPY Y-1 receptor antagonists: Influence of structurally diverse acyl substituents on stability and affinity. BIOORGANIC & MEDICINAL CHEMISTRY, 18 (17). pp. 6292-6304. ISSN 0968-0896,
Full text not available from this repository. (Request a copy)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 (Y1R) antagonism, Y1R 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 (Y1R antagonism) varied from low nM to one-digit mu M. 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. (C) 2010 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HISTAMINE H-2-RECEPTOR AGONISTS; NEUROPEPTIDE-Y; HIGHLY POTENT; IMIDAZOLYLPROPYLGUANIDINES; PHARMACOLOGY; GUANIDINES; INHIBITION; REACTIVITY; LIGANDS; ROUTE; Acyl guanidines; NPY; BIBP 3226; GPCR |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 13 Jul 2020 10:00 |
| Last Modified: | 13 Jul 2020 10:00 |
| URI: | https://pred.uni-regensburg.de/id/eprint/24204 |
Actions (login required)
 |
View Item |
