169203-64-9Relevant academic research and scientific papers
Balanced AT1/AT2 receptor antagonists. 4. XR510 and related 5-(3- amidopropanoyl)imidazoles possessing equal affinity for the AT1 and AT2 receptors
Quan,Chin,Ellis,Wong,Wexler,Timmermans
, p. 2938 - 2945 (1995)
The identification of the AT1 and AT2 receptor subtypes has stimulated interest in developing balanced angiotensin II receptor antagonists. A series of 5-(3-amidopropanoyl)imidazoles has been prepared which possess balanced affinity for the AT1 and AT2 receptors. XR510 (1), 1-[[2'- [[(isopentoxycarbonyl)amino]sulfonyl]-3-fluoro(1,1'-biphenyl)-4-yl]methyl]- 5-[3-(N-pyridin-3-ylbutanamido)propanoyl]-4-ethyl-2-propyl-1H-imidazole, potassium salt, exhibits subnanomolar affinity for both receptor sites. XR510 is very active in lowering blood pressure in renal hypertensive rats and furosemide-treated dogs following oral administration.
Imidazole 5-position substituted angiotensin II antagonists
-
, (2008/06/13)
Novel substituted imidazoles of Formula (III), which are useful as angiotensin-II antagonists, are disclosed: STR1 These compounds, exemplified by the compound 1-((2'-((i-Amyloxycarbonylamino)sulfonyl)-3-fluoro-(1,1'-biphenyl)-4-yl)methyl)-5-[2-(N-butyryl-N-pyridin-3-ylamino) ethylcarbonyl]-4-ethyl-2-propyl-1H-imidazole, are useful as antihypertensive agents.
