RT info:eu-repo/semantics/article
T1 Kynurenamines as Neural Nitric Oxide Synthase Inhibitors
A1 Entrena, Antonio
A1 Camacho, M. Encarnación
A1 Carrión, M. Dora
A1 López-Cara, Luisa C.
A1 Velasco, Guillermo
A1 León, Josefa
A1 Escames, Germaine
A1 Acuña Castroviejo, Darío
A1 Tapias, Víctor
A1 Gallo, Miguel A.
A1 Vivó, Antonio
A1 Espinosa, Antonio
AB To find new compounds with potential neuroprotective activity, we have designed, synthesized, and characterized a series of neural nitric oxide synthase (nNOS) inhibitors with a kynurenamine structure. Among them, N-[3-(2-amino-5-methoxyphenyl)-3-oxopropyl]acetamide is the main melatonin metabolite in the brain and shows the highest activity in the series, with an inhibition percentage of 65% at a 1 mM concentration. The structure-activity relationship of the new series partially reflects that of the previously reported 2-acylamido-4-(2-amino-5-methoxyphenyl)-4-oxobutyric acids, endowed with a kynurenine-like structure. Structural comparisons between these new kinurenamine derivatives, kynurenines, and 1-acyl-3-(2-amino-5-methoxyphenyl)-4,5-dihydro-1H-pyrazole derivatives also reported confirm our previous model for the nNOS inhibition.
SN 0022-2623
YR 2005
FD 2005
LK https://uvadoc.uva.es/handle/10324/63867
UL https://uvadoc.uva.es/handle/10324/63867
LA eng
NO Journal of Medicinal Chemistry, Dicembre 2005, vol. 48, n. 26, p. 8174-8181
NO Producción Científica
DS UVaDOC
RD 08-ago-2024