89075-08-1Relevant academic research and scientific papers
Bicycle compounds, processes for their preparation and pharmaceutical formulations containing compounds
-
, (2008/06/13)
Compounds of formula (I'), and compositions containing them: STR1 wherein n is 1, 2 or 3, each R1 independently represents a halogen atom; a hydroxy, carboxyl or C1-4 alkyl group, a C2-4 alkenyloxy, phenyl or phenyl-C
Structure-activity relationships of arylimidazopyridine cardiotonics: Discovery and inotropic activity of 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H-imidazo[4,5-c]pyridine
Robertson,Beedle,Krushinski,Pollock,Wilson,Wyss,Hayes
, p. 717 - 727 (2007/10/02)
Recently several noncatecholamine, nonglycoside cardiotonic drugs have been discovered that possess both inotropic and vasodilator activities in experimental animals and man. Prototypical compounds include amrinone, sulmazole, and fenoximone. We investigated the structural requirements necessary for optimal inotropic activity in a series of molecules containing a heterocyclic ring fused to 2-phenylimidazole and discovered that 2-phenylimidazo[4,5-c]pyridines were generally 5-10-fold more potent than analogous 2-phenylimidazo[4,5-b]pyridines (e.g., sulmazole) or 8-phenylpurines. Furthermore, all imidazo[4,5-c]pyridine analogues we tested were orally active; in contrast, only one of the imidazo[4,5-b]pyridine derivatives, sulmazole, was significantly active. One of several highly active compounds in the [4,5-c] series was 50 (LY175326, 2-[2-methoxy-4-(methylsulfinyl)phenyl]-1H- imidazo[4,5-c]pyridine hydrochloride). The structure-activity relationship of this series is presented and compared to that of the imidazo[4,5-b]pyridine and purine series.
