Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists.

Stafford, Jeffrey A; Pacofsky, Gregory J; Cox, Richard F; Cowan, Jill R; Dorsey, George F; Gonzales, Stephen S; Jung, David K; Koszalka, George W; McIntyre, Maggie S; Tidwell, Jeffrey H; Wiard, Robert P; Feldman, Paul L

Stafford, Jeffrey A; Pacofsky, Gregory J; Cox, Richard F; Cowan, Jill R; Dorsey, George F; Gonzales, Stephen S; Jung, David K; Koszalka, George W; McIntyre, Maggie S; Tidwell, Jeffrey H; Wiard, Robert P; Feldman, Paul L.

Afiliación

Stafford JA; GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.

Bioorg Med Chem Lett ; 12(21): 3215-8, 2002 Nov 04.

Article en En | MEDLINE | ID: mdl-12372537

ABSTRACT

ABSTRACT

The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles. Copyright2000 Elsevier Science Ltd.

Asunto(s)

Benzodiazepinas/síntesis química; Benzodiazepinas/farmacología; Agonistas de Receptores de GABA-A; Animales; Benzodiazepinas/farmacocinética; Cromatografía Líquida de Alta Presión; Humanos; Equilibrio Postural/efectos de los fármacos; Ratas; Receptores de GABA-A/metabolismo; Relación Estructura-Actividad

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Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Benzodiazepinas / Agonistas de Receptores de GABA-A Tipo de estudio: Diagnostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2002 Tipo del documento: Article País de afiliación: Estados Unidos

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