Synthesis and pharmacological characterization of 2-(acylamino)thiophene derivatives as metabolically stable, orally effective, positive allosteric modulators of the GABAB receptor

Journal of Medicinal Chemistry

Volumn 56, Issue 9, 2013, Pages 3620-3635

  Mugnaini, Claudia ^a   Pedani, Valentina ^a   Casu, Angelo ^b   Lobina, Carla ^c   Casti, Alberto ^b   MacCioni, Paola ^c   Porcu, Alessandra ^b   Giunta, Daniela ^c   Lamponi, Stefania ^a   Solinas, Maurizio ^c   Dragoni, Stefania ^d   Valoti, Massimo ^a   Colombo, Giancarlo ^c   Castelli, Maria Paola ^b   Gessa, Gian Luigi ^c   Corelli, Federico ^a  

^a UNIVERSITY OF SIENA   (Italy)

^b UNIVERSITY OF CAGLIARI   (Italy)

^c CNR   (Italy)

^d UNIVERSITY OF PERUGIA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

2 (ACYLAMINO)THIOPHENE DERIVATIVE; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; BACLOFEN; BHF 177; COR 627; COR 628; METHYL 2 [[(4 CHLOROPHENYL)CARBONYL]AMINO] 4 ETHYL 5 METHYLTHIOPHENE 3 CARBOXYLATE; METHYL 2 [[(4 TERT BUTYLPHENYL)CARBONYL)AMINO] 4 ETHYL 5 METHYLTHIOPHENE 3 CARBOXYLATE; METHYL 4 ETHYL 5 METHYL 2 [[(4 METHYLPHENYL)CARBONYL)AMINO]THIOPHENE 3 CARBOXYLATE; METHYL 4 ETHYL 5 METHYL 2 [[(4 TRIFLUOROMETHYLPHENYL)CARBONYL]AMINO]THIOPHENE 3 CARBOXYLATE; N,N' DICYCLOPENTYL 2 METHYLTHIO 5 NITRO 4,6 PYRIMIDINEDIAMINE; THIOPHENE; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG EFFICACY; DRUG POTENCY; DRUG STABILITY; DRUG STRUCTURE; DRUG SYNTHESIS; HYPNOSIS; MOUSE; NONHUMAN; SEDATION;

ADMINISTRATION, ORAL; ALLOSTERIC REGULATION; ANIMALS; BACLOFEN; CHEMISTRY TECHNIQUES, SYNTHETIC; DRUG DESIGN; DRUG STABILITY; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); IMMOBILITY RESPONSE, TONIC; MICE; MICROSOMES, LIVER; NIH 3T3 CELLS; PENTOBARBITAL; RATS; RECEPTORS, GABA-B; THIOPHENES;

EID: 84877693067     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm400144w     Document Type: Article

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