Benzodiazepine receptor ligands. 8: Synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: High affinity ligands endowed with inverse-agonist pharmacological efficacy

Bioorganic and Medicinal Chemistry

Volumn 14, Issue 3, 2006, Pages 758-775

  Guerrini, Gabriella ^a   Costanzo, Annarella ^a   Ciciani, Giovanna ^a   Bruni, Fabrizio ^a   Selleri, Silvia ^a   Costagli, Camilla ^a   Besnard, François ^b   Costa, Barbara ^c   Martini, Claudia ^c   De Siena, Gaetano ^a   Malmberg Aiello, Petra ^a  

^a UNIVERSITY OF FLORENCE   (Italy)

^b SANOFI   (France)

^c UNIVERSITY OF PISA   (Italy)

Author keywords

GABAA BzR complex ligands; Inverse agonists; Pyrazolo 5,1 c 1,2,4 benzotriazines; Tricyclic heteroaromatic system

Indexed keywords

3 (2 FURYLMETHOXYCARBONYL) 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 BROMOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 ETHOXYPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 IODOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 METHOXYPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 METHOXYBENZYLOXYCARBONYL) 8 METHYLTHIOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 NITROBENZYLOXYCARBONYL) 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 BROMOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 ETHOXYPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 IODOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 METHOXYPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (2 THIENYLMETHOXYCARBONYL) 8 METHYLTHIOPYRAZOLO[5,1 C][1,2,4] BENZOTRIAZINE 5 OXIDE; 3 (3 THIENYLMETHOXYCARBONYL) 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (THIEN 3 YL) 8 BROMOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 (THIEN 3 YL) 8 ETHOXYPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 BENZYLOXYCARBONYL 8 METHYLPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 ETHOXYCARBONYL 8 BROMOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 3 ETHOXYCARBONYL 8 IODOPYRAZOLO[5,1 C][1,2,4]BENZOTRIAZINE 5 OXIDE; 4 AMINOBUTYRIC ACID A RECEPTOR; ALCOHOL; BENZODIAZEPINE RECEPTOR; BENZODIAZEPINE RECEPTOR INVERSE STIMULATING AGENT; DIAZEPAM; FLUMAZENIL; PYRAZOLE DERIVATIVE; TRIAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZOLPIDEM;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICONVULSANT ACTIVITY; ARTICLE; BINDING ASSAY; CONTROLLED STUDY; CONVULSION; COW; DRUG EFFECT; DRUG MECHANISM; DRUG POTENTIATION; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SELECTIVITY; DRUG SYNTHESIS; ELECTRON; EMBRYO; HUMAN; HUMAN CELL; IN VIVO STUDY; LIPOPHILICITY; MALE; MOTOR ACTIVITY; MOTOR COORDINATION; MOUSE; MUSCLE RELAXATION; NONHUMAN; RAT; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION; TRANQUILIZING ACTIVITY;

ANIMALS; ANTI-ANXIETY AGENTS; ANTICONVULSANTS; ANXIETY; BINDING, COMPETITIVE; BRAIN; CATTLE; FLUMAZENIL; LIGANDS; MALE; MICE; MOTOR ACTIVITY; MUSCLE RELAXATION; RATS; RATS, WISTAR; RECEPTORS, GABA-A; SLEEP; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZINES;

ANIMALIA;

EID: 28844436061     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2005.08.058     Document Type: Article

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