132287-48-0Relevant academic research and scientific papers
AROMATASE INHIBITING 4(5)-IMIDAZOLES
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, (2008/06/13)
Imidazole derivatives of the formula: where in R1, R2, R1 and R2 which can be the same or different, are H, CH3, C2 H5, OCH3, OH, CH2 OH, NH2 or halogen; R' if H or where R3 is H, CH3, or halogen; R4 is H and R5 is H or OH and R6 is H or OH or one of R5 and R6 is H and the other, together with R4, forms a bond and X and Y, which can be the same or different, are a bond, a straight C1-2 -alkyl or the corresponding alkenyl, and pharmaceutically acceptable salts thereof exhibit valuable pharmacological properties, especially aromatase inhibiting effects and are useful in the treatment of estrogen dependent diseases, e.g. breast cancer. Anti-mycotic and antifungal properties have also been found.
Synthesis and structure-activity of 4(5)-(2,2-diphenylethyl)imidazoles as new α2-adrenoreceptor antagonists
Cordi,Snyers,Giraud-Mangin,Van der Maesen,Van Hoeck,Beuze,Ellens,Napora,Gillet,Gorissen,Calderon,Remacle,Janssens de Varebeke,Van Dorsser,Roba
, p. 557 - 568 (2007/10/02)
4(5)-(2,2-diphenylethyl)imidazole 6a is described as being a potent (pK(i) = 8.16 for displacement of [3H] p-aminoclonidine) and selective (selectivity = -log (pK(i) α2 - pK(i) α1) = 81) α2-adrenoreceptor antagonist (pA2 = 8.73 versus clonidine in the electrically stimulated guinea pig ileum) with additional activity as a norepinephrine uptake inhibitor (IC50 = 0.3 μM). An investigation of the structure-activity relationships of compounds closely related to 6a has been carried out. This included substitution of the phenyl and imidazole rings and modification of the link between these two ring systems. The various synthetic routes used are described. The affinity and the selectivity of the compounds for the α2 site were determined by studying the displacement of [3H] p-aminoclonidine and [3H] WB-4101 from rat forebrain membranes. The efficacy of the compounds was defined by measuring the antagonism of the clonidine effect on the electrically stimulated guinea pig ileum.
