Cinelli, Maris A. published the artcileFirst Contact: 7-Phenyl-2-Aminoquinolines, Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors That Target an Isoform-Specific Aspartate, Recommanded Product: (S)-2-Methylpropane-2-sulfinamide, the main research area is phenyl aminoquinoline preparation neuronal nitric oxide synthase inhibitor human; mol docking SAR phenyl aminoquinoline crystal structure.
Inhibition of neuronal nitric oxide synthase (nNOS), an enzyme implicated in neurodegenerative disorders, is an attractive strategy for treating or preventing these diseases. Several classes of 2-aminoquinoline-based nNOS inhibitors were developed previously, but these compounds had drawbacks including off-target promiscuity, low activity against human nNOS, and only modest selectivity for nNOS over related enzymes. In this study, new nNOS inhibitors based on 7-phenyl-2-aminoquinoline were synthesized and assayed them against rat and human nNOS, human eNOS, and murine and (in some cases) human iNOS. Compounds with a meta-relationship between the aminoquinoline and a pos. charged tail moiety were potent and had up to nearly 900-fold selectivity for human nNOS over human eNOS. X-ray crystallog. indicates that the amino groups of some compounds occupy a water-filled pocket surrounding an nNOS-specific aspartate residue (absent in eNOS). This interaction was confirmed by mutagenesis studies, making 7-phenyl-2-aminoquinolines the first aminoquinolines to interact with this residue.
Journal of Medicinal Chemistry published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Recommanded Product: (S)-2-Methylpropane-2-sulfinamide.
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