| Autor: |
Lolli ML; Dipartimento di Scienza e Tecnologia del Farmaco, Università degli Studi di Torino, Via Pietro Giuria 9, 10125 Torino, Italy., Hansen SL, Rolando B, Nielsen B, Wellendorph P, Madsen K, Larsen OM, Kristiansen U, Fruttero R, Gasco A, Johansen TN |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2006 Jul 13; Vol. 49 (14), pp. 4442-6. |
| DOI: |
10.1021/jm051288b |
| Abstrakt: |
Three 4-substituted 1,2,5-oxadiazol-3-ols containing aminoalkyl substituents (analogues and homologues of gamma-aminobutyric acid (GABA)) were synthesized to investigate the hydroxy-1,2,5-oxadiazolyl moiety as a bioisoster for a carboxyl group at GABA receptors. The pK(a) values of the target compounds were close to those of GABA. At GABA(A) receptors of cultured cerebral cortical neurons, weak agonist and partial agonist profiles were identified, demonstrating the 4-hydroxy-1,2,5-oxadiazol-3-yl unit to be a nonclassical carboxyl group bioisoster. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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