Inotropic "A" ring substituted sulmazole and isomazole analogues.
J Med Chem
; 33(8): 2231-9, 1990 Aug.
Article
em En
| MEDLINE
| ID: mdl-2165165
ABSTRACT
A series of "A" ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pKA's, protonation sites, and log P values were measured for selected compounds and their electronic properties were calculated. No simple correlation between inotropic activity and pKA, protonation site, or log P value was observed. However, in vitro inotropism did correlate with the calculated charge density of the "B" ring imidazo nitrogen atom. The 6-position of sulmazole appeared to be the most tolerant toward substituents, the 6-amino derivative 7 being a more potent inotrope than sulmazole itself. 4-Methoxyisomazole 13 had comparable in vivo inotropic properties to those of isomazole.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Cardiotônicos
/
Imidazóis
/
Contração Miocárdica
Limite:
Animals
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
1990
Tipo de documento:
Article
País de afiliação:
Reino Unido