Synthesis and biological evaluation as AChE inhibitors of new indanones and thiaindanones related to donepezil

European Journal of Medicinal Chemistry

Volumn 40, Issue 12, 2005, Pages 1222-1245

  Omran, Ziad ^a   Cailly, Thomas ^a   Lescot, Elodie ^a   Santos, Jana Sopkova De Oliveira ^a   Agondanou, Jean Hugues ^a   Lisowski, Vincent ^a   Fabis, Frédéric ^a   Godard, Anne Marie ^a   Stiebing, Silvia ^a   Le Flem, Guillaume ^a   Boulouard, Michel ^a   Dauphin, François ^a   Dallemagne, Patrick ^a   Rault, Sylvain ^a  

^a CENTRE D ETUDES ET DE RECHERCHE SUR LE MÉDICAMENT DE NORMANDIE   (France)

Author keywords

Acetylcholinesterase; Alzheimer disease; Cyclopentathiophene; Donepezil; Indanone; Thiaindanone

Indexed keywords

2 (4 BENZYLPIPERAZIN 1 YL) N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 (4 BENZYLPIPERIDIN 1 YL) N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (2 BROMOBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2 CHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2 CHLOROBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (2 FLUOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2 IODOBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2 METHYLBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2 NITROBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (2 TRIFLUOROMETHYLBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2,3 DICHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2,4 DICHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2,5 DICHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2,6 DICHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (2,6 DICHLOROBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (3 CHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (3 CHLOROBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (3 CYANOBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (3 FLUOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (3 TRIFLUOROMETHYLBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (4 BROMOBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (4 CHLOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (4 CHLOROBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; 2 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL] N (1,3 DIBROMO 6 OXO 5,6 DIHYDRO 4H CYCLOPENTA[C]THIEN 4 YL)ACETAMIDE; 2 [4 (4 METHOXYBENZYL)PIPERAZIN 1 YL] N (5,6 DIMETHOXY 3 OXO 2,3 DIHYDRO 1H INDEN 1 YL)ACETAMIDE; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; DONEPEZIL; INDANONE DERIVATIVE; THIAINDANONE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; COMPARATIVE STUDY; DRUG ACTIVITY; DRUG MECHANISM; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; IC 50; IN VITRO STUDY;

CHOLINESTERASE INHIBITORS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; INDANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PIPERIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 27744484135     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2005.07.009     Document Type: Article

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