4,5-Dihydro-1H-pyrazole Derivatives with Inhibitory nNOS Activity in Rat Brain: Synthesis and Structure−Activity Relationships
Journal of Medicinal Chemistry2004Vol. 47(23), pp. 5641–5650
Citations Over TimeTop 19% of 2004 papers
M. Encarnación Camacho, Josefa León, Antonio Entrena, Guillermo Velasco, María Dora Carriòn, Germaine Escames, Antonio De Vivo, Darío Acuña‐Castroviejo, Miguel Á. Gallo, Antonio Espinosa
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.
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