Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimers Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography

Journal of Medicinal Chemistry

Volumn 59, Issue 1, 2016, Pages 114-131

  Zha, Xiaoming ^a   Lamba, Doriano ^b   Zhang, Lili ^a   Lou, Yinghan ^a   Xu, Changxu ^a   Kang, Di ^a   Chen, Li ^a   Xu, Yungen ^a   Zhang, Luyong ^a   De Simone, Angela ^a   Samez, Sarah ^b,d   Pesaresi, Alessandro ^b   Stojan, Jure ^e   Lopez, Manuela G ^f   Egea, Javier ^f   Andrisano, Vincenza ^c   Bartolini, Manuela ^c  

^a CHINA PHARMACEUTICAL UNIVERSITY   (China)

^b CNR   (Italy)

^c UNIVERSITY OF BOLOGNA   (Italy)

^d UNIVERSITY OF TRIESTE   (Italy)

^e UNIVERSITY OF LJUBLJANA   (Slovenia)

^f INSTITUTO TEÓFILO HERNANDO   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

7 METHOXY N [6 [(1,2,3,4 TETRAHYDROACRIDIN 9 YL)AMINO]HEXYL]BENZOFURAN 2 CARBOXAMIDE; 7 METHOXY N [6 [(7,8,9,10 TETRAHYDRO 6H CYCLOHEPTA[B]QUINOLIN 11 YL)AMINO]HEXYL]BENZOFURAN 2 CARBOXAMIDE; 7 METHOXY N [7 [(1,2,3,4 TETRAHYDROACRIDIN 9 YL)AMINO]HEPTYL]BENZOFURAN 2 CARBOXAMIDE; ACETYLCHOLINESTERASE; AMYLOID BETA PROTEIN; BENZOFURAN DERIVATIVE; CHOLINESTERASE; LIGAND; N 1 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL) N 6 [(7 METHOXY BENZOFURAN 2 YL)METHYL]HEXANE 1,6 DIAMINE; N 1 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL) N 6 [[(7 METHOXYBENZOFURAN 2 YL)METHYOXY BENOFURAN 2 YL]METHYL]HEXANE 1,6 DIAMINE; N 1 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL) N 6, N 6 BIS[(7 METHOXYBENZOFURAN 2 YL)METHYL]HEXANE 1,6 DIAMINE; N 1 (BENZOFURAN 2 YLMETHYL) N 6 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)HEXANE 1,6 DIAMINE; N 1 (BENZOFURAN 2 YLMETHYL) N 7 (1,2,3,4 TETRAHYDROACRIDIN 9 YL)HEPTANE 1,7 DIAMINE; N 1 (BENZOFURAN 2 YLMETHYL) N 7 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)HEPTANE 1,7 DIAMINE; N 1 [(7 METHOXYBENZOFURAN 2 YL)METHYL] N 6 (1,2,3,4 TETRAHYDROACRIDIN 9 YL)HEXANE 1,6 DIAMINE; N 1 [(7 METHOXYBENZOFURAN 2 YL)METHYL] N 7 (7,8,9,10 TETRAHYDRO 6H CYCLOHEPTA[B]QUINOLIN 11 YL)HEPTANE 1,7 DIAMINE; N 1, N 1 BIS(BENZOFURAN 2 YLMETHYL) N 6 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)HEXANE 1,6 DIAMINE; N 1, N 1 BIS[(7 METHOXYBENZOFURAN 2 YL)METHYL] N 6 (1,2,3,4 TETRAHYDROACRIDIN 9 YL)HEXANE 1,6 DIAMINE; N 1, N 1 BIS[(7 METHOXYBENZOFURAN 2 YL)METHYL] N 6 (7,8,9,10 TETRAHYDRO 6H CYCLOHEPTA[B]QUINOLIN 11 YL)HEXANE 1,6 DIAMINE; N [(1,2,3,4 TETRAHYDROACRIDIN 9 YLAMINO)METHYL]BENZOFURAN 2 CARBOXAMIDE; N [6 [(2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)AMINO]HEXYL] 7 METHOXYBENZOFURAN 2 CARBOXAMIDE; N [6 [(2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)AMINO]HEXYL]BENZOFURAN 2 CARBOXAMIDE; N [6 [(7,8,9,10 TETRAHYDRO 6H CYCLOHEPTA[B]QUINOLIN 11 YL)AMINO]HEXYL]BENZOFURAN 2 CARBOXAMIDE; N [7 (2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YLAMINO)HEPTYL] 7 METHOXYBENZOFURAN 2 CARBOXAMIDE; N [7 (7,8,9,10 TETRAHYDRO 6H CYCLOHEPTA[B]QUINOLIN 11 YLAMINO)HEPTYL] 7 METHOXYBENZOFURAN 2 CARBOXAMIDE; N [7 (7,8,9,10 TETRAHYDRO 6H CYCOHEPTA[B]QUINOLIN 11 YLAMINO)HEPTYL]BENZOFURAN 2 CARBOXAMIDE; N [7 [(1,2,3,4 TETRAHYDROACRIDIN 9 YL)AMINO]HEPTYL]BENZOFURAN 2 CARBOXAMIDE; N [7 [(2,3 DIHYDRO 1H CYCLOPENTA[B]QUINOLIN 9 YL)AMINO]HEPTYL]BENZOFURAN 2 CARBOXAMIDE; SCOPOLAMINE; TACRINE; UNCLASSIFIED DRUG; ASPARTIC PROTEINASE; BACE1 PROTEIN, HUMAN; CHOLINESTERASE INHIBITOR; NOOTROPIC AGENT; SECRETASE;

ALZHEIMER DISEASE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG SYNTHESIS; DRUG TARGETING; HUMAN; IC50; KINETIC PARAMETERS; LIVER TOXICITY; MALE; MOUSE; NONHUMAN; PROTEIN AGGREGATION; X RAY CRYSTALLOGRAPHY; ANIMAL; ANIMAL BEHAVIOR; ANTAGONISTS AND INHIBITORS; CELL LINE; CELL SURVIVAL; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; INSTITUTE FOR CANCER RESEARCH MOUSE; PATHOLOGY; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TORPEDO; TOXIC HEPATITIS;

ALZHEIMER DISEASE; AMYLOID PRECURSOR PROTEIN SECRETASES; ANIMALS; ASPARTIC ACID ENDOPEPTIDASES; BEHAVIOR, ANIMAL; BENZOFURANS; CELL LINE; CELL SURVIVAL; CHOLINESTERASE INHIBITORS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; DRUG-INDUCED LIVER INJURY; HUMANS; MALE; MICE; MICE, INBRED ICR; MODELS, MOLECULAR; NOOTROPIC AGENTS; STRUCTURE-ACTIVITY RELATIONSHIP; TACRINE; TORPEDO;

EID: 84955134350     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b01119     Document Type: Article

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