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Carrión, M. Dora López Cara, Luisa C. Camacho, M. Encarnación Tapias Molina, Victor Escames, Germaine Acuña Castroviejo, Darío Espinosa, Antonio Gallo, Miguel A. Entrena, Antonio 2024-01-01T20:54:55Z 2024-01-01T20:54:55Z 2008 9999-01-01 European Journal of Medicinal Chemistry, Noviembre 2008, vol. 43, n. 11, p. 2579-2591 0223-5234 https://uvadoc.uva.es/handle/10324/63871 10.1016/j.ejmech.2008.01.014 2579 11 2591 European Journal of Medicinal Chemistry 43 Producción Científica 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. This work was partially supported by grants from the Ministerio de Ciencia y Tecnología (SAF2005-07991-C02-01 and SAF2005-07991-C02-02) and from the Junta de Andalucía (P06-CTS-01941). application/pdf eng info:eu-repo/semantics/embargoedAccess Pyrazoles and pyrazolines as neural and inducible nitric oxide synthase (nNOS and iNOS) potential inhibitors (III) info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion SI