RESUMO
A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4).
Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Amidas/uso terapêutico , Antiasmáticos/uso terapêutico , Asma/tratamento farmacológico , Inibidores de Fosfodiesterase/uso terapêutico , Amidas/farmacologia , Antiasmáticos/farmacologia , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Humanos , Inibidores de Fosfodiesterase/farmacologiaRESUMO
The synthesis and pharmacological profile of a novel series of 2-substituted 8-methoxyquinolines is described. The 2-trifluoromethyl compound was found to be a potent inhibitor of phosphodiesterase type 4 (PDE4).
Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Inibidores de Fosfodiesterase/síntese química , Inibidores de Fosfodiesterase/farmacologia , Quinolinas/síntese química , Quinolinas/farmacologia , Animais , Área Sob a Curva , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Cobaias , Inibidores de Fosfodiesterase/farmacocinética , Quinolinas/farmacocinética , Vômito/induzido quimicamenteRESUMO
The syntheses and pharmacological profiles of some 2-trifluoromethyl-8-methoxyquinoline-5-carboxamides are described. SCH351591 is a potent selective inhibitor of phosphodiesterase type 4 (PDE4).
Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Óxidos N-Cíclicos/síntese química , Óxidos N-Cíclicos/farmacologia , Inibidores de Fosfodiesterase/síntese química , Inibidores de Fosfodiesterase/farmacologia , Quinolinas/síntese química , Quinolinas/farmacologia , Animais , Área Sob a Curva , Óxidos N-Cíclicos/farmacocinética , Nucleotídeo Cíclico Fosfodiesterase do Tipo 4 , Cobaias , Inibidores de Fosfodiesterase/farmacocinética , Quinolinas/farmacocinéticaRESUMO
The synthesis and pharmacological profile of a novel series of 7-methoxy-furo[2,3-c]pyridine-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4).