Themanagementofneurologicaldisordershavehugeandincreasinghumanandeconomiccosts.Despitethis,thereisascarcityofeffectivetherapeutics,andthereisanextremeurgencyfornewandrealtreatments.Inthisshortreviewweanalyzesomepromisingadvancementsinthesearchofnewbioactivemoleculestargetingneuronalnitricoxidesynthase(nNOS),anenzymedeputedtothebiosynthesisofnitricoxide(NO).Indifferentconditionsofneuronaldamages,thismoleculeisoverproduced,contributingtothepathogenesisandprogressionofneuronaldiseases.TwomainapproachestomodulatenNOSarediscussed:afirstoneconsistinginthedirectinhibitionoftheenzymebymeansofsmallorganicmolecules,whichcanbealsoactiveagainstotherdifferenttargetsinvolvedinsuchdiseases.AsecondsectionisdedicatedtomoleculesabletopreventtheformationoftheternarycomplexN-methyl-D-aspartate(NMDA)-typeglutamatereceptors,postsynapticdensity-95(PSD95)protein-nNOS,whichisnecessarytoactivatethelatterforthebiosynthesisofNO.
