127382-95-0Relevant articles and documents
Inotropic 'A' ring substituted sulmazole and isomazole analogues
Barraclough,Black,Cambridge,Collard,Firmin,Gerskowitch,Glen,Giles,Hill,Hull,Iyer,King,Kneen,Lindon,Nobbs,Randall,Shah,Smith,Vine,et al.
, p. 2231 - 2239 (2007/10/02)
A series of 'A' ring substituted sulmazole and isomazole analogues have been prepared and evaluated as inotropic agents. pK(A)'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 pK(A), 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, th 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.
