RT info:eu-repo/semantics/article
T1 Pyrazoles and pyrazolines as neural and inducible nitric oxide synthase (nNOS and iNOS) potential inhibitors (III)
A1 Carrión, M. Dora
A1 López Cara, Luisa C.
A1 Camacho, M. Encarnación
A1 Tapias, Víctor
A1 Escames, Germaine
A1 Acuña Castroviejo, Darío
A1 Espinosa, Antonio
A1 Gallo, Miguel A.
A1 Entrena, Antonio
AB We have previously described a series of 4,5-dihydro-1H-pyrazole as moderately potent nNOS inhibitors. As a follow up of these studies, we report here the preparation and the preliminary evaluation of a series of 1-alkyl-3-benzoyl-4,5-dihydro-1H-pyrazole and 1-alkyl-3-benzoyl-1H-pyrazole as potential inhibitors of both neuronal and inducible nitric oxide synthases (nNOS and iNOS). None of the reported compounds exhibited significant iNOS or nNOS inhibition, although the 1-benzyl-3-(2-amino-5-chlorobenzoyl)-1H-pyrazole-5-carboxylic acid ethyl ester derivative (10l), which shows an inhibition of 50% versus iNOS at a 1mM final concentration and no activity against nNOS, is potentially amenable of further optimization. The reasons for the inactivity of the reported series are discussed on the basis of docking studies.
SN 0223-5234
YR 2008
FD 2008
LK https://uvadoc.uva.es/handle/10324/63871
UL https://uvadoc.uva.es/handle/10324/63871
LA eng
NO European Journal of Medicinal Chemistry, Noviembre 2008, vol. 43, n. 11, p. 2579-2591
NO Producción Científica
DS UVaDOC
RD 17-jul-2024