Pubmed-entry ::= {
  pmid 22243648,
  medent {
    em std {
      year 2012,
      month 2,
      day 9
    },
    cit {
      title {
        name "New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents
 for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and
 beta-amyloid-reducing properties."
      },
      authors {
        names ml {
          "Fernandez-Bachiller MI",
          "Perez C",
          "Monjas L",
          "Rademann J",
          "Rodriguez-Franco MI"
        },
        affil str "Instituto de Quimica Medica, Consejo Superior de
 Investigaciones Cientificas (IQM-CSIC), Juan de la Cierva 3, 28006 Madrid,
 Spain."
      },
      from journal {
        title {
          iso-jta "J. Med. Chem.",
          ml-jta "J Med Chem",
          issn "1520-4804",
          name "Journal of medicinal chemistry"
        },
        imp {
          date std {
            year 2012,
            month 2,
            day 9
          },
          volume "55",
          issue "3",
          pages "1303-1317",
          language "eng",
          pubstatus ppublish,
          history {
            {
              pubstatus aheadofprint,
              date std {
                year 2012,
                month 1,
                day 27
              }
            },
            {
              pubstatus other,
              date std {
                year 2012,
                month 1,
                day 17,
                hour 6,
                minute 0
              }
            },
            {
              pubstatus pubmed,
              date std {
                year 2012,
                month 1,
                day 17,
                hour 6,
                minute 0
              }
            },
            {
              pubstatus medline,
              date std {
                year 2012,
                month 4,
                day 24,
                hour 6,
                minute 0
              }
            }
          }
        }
      },
      ids {
        doi "10.1021/jm201460y",
        pubmed 22243648
      }
    },
    abstract "By using fragments endowed with interesting and complementary
 properties for the treatment of Alzheimer's disease (AD), a new family of
 tacrine-4-oxo-4H-chromene hybrids has been designed, synthesized, and
 evaluated biologically. The tacrine fragment was selected for its inhibition
 of cholinesterases, and the flavonoid scaffold derived from 4-oxo-4H 
 -chromene was chosen for its radical capture and beta-secretase 1 (BACE-1)
 inhibitory activities. At nano- and picomolar concentrations, the new
 tacrine-4-oxo-4H-chromene hybrids inhibit human acetyl- and
 butyrylcholinesterase (h-AChE and h-BuChE), being more potent than the parent
 inhibitor, tacrine. They are also potent inhibitors of human BACE-1, better
 than the parent flavonoid, apigenin. They show interesting antioxidant
 properties and could be able to penetrate into the CNS according to the in
 vitro PAMPA-BBB assay. Among the hybrids investigated, 6-hydroxy-4-oxo-
 N-{10-[(1,2,3,4-tetrahydroacridin-9-yl)amino]decyl}-4
 H-chromene-2-carboxamide (19) shows potent combined inhibition of human
 BACE-1 and ChEs, as well as good antioxidant and CNS-permeable properties.",
    mesh {
      {
        term "Acetylcholinesterase",
        qual {
          {
            subh "chemistry"
          }
        }
      },
      {
        term "Alzheimer Disease",
        qual {
          {
            mp TRUE,
            subh "drug therapy"
          }
        }
      },
      {
        term "Amyloid Precursor Protein Secretases",
        qual {
          {
            subh "antagonists & inhibitors"
          }
        }
      },
      {
        term "Amyloid beta-Peptides",
        qual {
          {
            mp TRUE,
            subh "metabolism"
          }
        }
      },
      {
        term "Animals"
      },
      {
        term "Antioxidants",
        qual {
          {
            mp TRUE,
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      },
      {
        term "Aspartic Acid Endopeptidases",
        qual {
          {
            subh "antagonists & inhibitors"
          }
        }
      },
      {
        term "Benzopyrans",
        qual {
          {
            mp TRUE,
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      },
      {
        term "Blood-Brain Barrier",
        qual {
          {
            subh "metabolism"
          }
        }
      },
      {
        term "Butyrylcholinesterase",
        qual {
          {
            subh "chemistry"
          }
        }
      },
      {
        term "Catalytic Domain"
      },
      {
        term "Cattle"
      },
      {
        term "Cholinesterase Inhibitors",
        qual {
          {
            mp TRUE,
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      },
      {
        term "Chromones",
        qual {
          {
            mp TRUE,
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      },
      {
        term "Free Radical Scavengers",
        qual {
          {
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      },
      {
        term "Humans"
      },
      {
        term "Membranes, Artificial"
      },
      {
        term "Permeability"
      },
      {
        term "Structure-Activity Relationship"
      },
      {
        term "Tacrine",
        qual {
          {
            mp TRUE,
            subh "analogs & derivatives"
          },
          {
            mp TRUE,
            subh "chemical synthesis"
          },
          {
            subh "chemistry"
          },
          {
            subh "pharmacology"
          }
        }
      }
    },
    substance {
      {
        type nameonly,
        name "6-hydroxy-4-oxo-N-(10-((1,2,3,4-tetrahydroacridin-9-yl)amino)dec
yl)-4H-chromene-2-carboxamide"
      },
      {
        type nameonly,
        name "Amyloid beta-Peptides"
      },
      {
        type nameonly,
        name "Antioxidants"
      },
      {
        type nameonly,
        name "Benzopyrans"
      },
      {
        type nameonly,
        name "Cholinesterase Inhibitors"
      },
      {
        type nameonly,
        name "Chromones"
      },
      {
        type nameonly,
        name "Free Radical Scavengers"
      },
      {
        type nameonly,
        name "Membranes, Artificial"
      },
      {
        type cas,
        cit "321-64-2",
        name "Tacrine"
      },
      {
        type ec,
        cit "3.1.1.-",
        name "Butyrylcholinesterase"
      },
      {
        type ec,
        cit "3.1.1.7",
        name "Acetylcholinesterase"
      },
      {
        type ec,
        cit "3.4.-",
        name "Amyloid Precursor Protein Secretases"
      },
      {
        type ec,
        cit "3.4.23.-",
        name "Aspartic Acid Endopeptidases"
      },
      {
        type ec,
        cit "3.4.23.46",
        name "BACE1 protein, human"
      }
    },
    pmid 22243648,
    pub-type {
      "Journal Article",
      "Research Support, Non-U.S. Gov't"
    },
    status medline
  }
}

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