2004•Journal of Medicinal ChemistryRequires access
4,5-Dihydro-1H-pyrazole Derivatives with Inhibitory nNOS Activity in Rat Brain: Synthesis and Structure−Activity Relationships
M. Encarnación Camacho, Josefa León, Antonio Entrena, Guillermo Velasco, María Dora Carriòn, Germaine Escames, Antonio De Vivo, Darı́o Acuña-Castroviejo, Miguel Á. Gallo, Antonio Espinosa
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Abstract
In an attempt to find new compounds with neuroprotective activity, we have designed, synthesized and characterized 19 new nNOS inhibitors with a 4,5-dihydro-1H-pyrazole structure. Compounds 11r [1-cyclopropanecarbonyl-3-(2-amino-5-chlorophenyl)-4,5-dihydro-1H-pyrazole] and 11e [1-cyclopropanecarbonyl-3-(2-amino-5-methoxyphenyl)- 4,5-dihydro-1H-pyrazole] show the highest activities with inhibition percentages of 70% and 62%, respectively. A structure-activity relationship for the nNOS inhibition can be established from the structural comparison of these new pyrazole derivatives and the described synthetic kynurenines 10.