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.

Afiliação

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

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

Article em 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.

Assuntos

Benzodiazepinas/síntese química; Benzodiazepinas/farmacologia; Agonistas de Receptores de GABA-A; Animais; Benzodiazepinas/farmacocinética; Cromatografia Líquida de Alta Pressão; Humanos; Equilíbrio Postural/efeitos dos fármacos; Ratos; Receptores de GABA-A/metabolismo; Relação Estrutura-Atividade

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Base de dados: MEDLINE Assunto principal: Benzodiazepinas / Agonistas de Receptores de GABA-A Idioma: En Ano de publicação: 2002 Tipo de documento: Article

Buscar no Google

Imprimir

XML

PubMed Links

Base de dados: MEDLINE Assunto principal: Benzodiazepinas / Agonistas de Receptores de GABA-A Idioma: En Ano de publicação: 2002 Tipo de documento: Article