17374-09-3Relevant academic research and scientific papers
Azole derivatives as histamine H3 receptor antagonists, Part 2: C-C and C-S coupled heterocycles
Walter,Isensee,Kottke,Ligneau,Camelin,Schwartz,Stark
scheme or table, p. 5883 - 5886 (2010/11/18)
With a small series of compounds we demonstrated the variability in the core region of the human histamine H3 receptor (hH3R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Additional variations achieved by coupling different residues to the heterocyclic core structure led to further optimisation of in vitro receptor binding of the novel azole derivatives.
Acyl-CoA::cholesterol O-Acyl Transferase (ACAT) Inhibitors. 1. 2-(Alkylthio)-4,5-diphenyl-1H-imidazoles as Potent Inhibitors of ACAT
Harris, Neil V.,Smith, Christopher,Asthon, Michael J.,Bridge, Andrew W.,Bush, Raymond C.,et al.
, p. 4384 - 4392 (2007/10/02)
A potent, bioavailable ACAT inhibitor may have beneficial effects in the treatment of atherosclerosis by (i) reducing the absorption of dietary cholesterol, (ii) reducing the secretion of very low density lipoproteins into plasma from the liver, and (iii) preventing the transformation of arterial macrophages into foam cells.We have found that a mevalonate derivative 2, which contains a 4,5-diphenyl-1H-imidazol-2-yl moiety, inhibits rat hepatic microsomal ACAT in vitro and produces a significant hypocholesterolemic effect in the cholesterol-fed rat.Structure-activity relationships for analogues of 2 demonstrate that the 4,5-diphenyl-1H-imidazole moiety is a pharmacophore for inhibition of rat microsomal ACAT.
