Methylated imidazole derivatives

One of the earliest indications of the potential of IL-based moieties for biomolecule separations may be found by examining the report of a methyl imidazole-derived phase in HPLC [60]. In this study, it was found that at a pH below its pfCg, the methyl imidazole-derived phase demonstrated enhanced... 

Methylated imidazole derivatives, imidazole acetic acid riboside (D 20) Urine... 

Miconazole. Miconazole nitrate [22832-87-7] (Fig. 2), the 1-phenethyl-imidazole derivative first described in 1969, interferes at low doses with the cytochrome P-450 dependent ergosterol biosynthesis in yeasts and fungi. The result is accumulation of C-14 methylated sterols on the one hand and reduction of the ergosterol levels in the membranes on the other hand (12). Analogous to clotrimazole, this leads to a disturbance in the membranes it results in inhibition of ceU repHcation, mycelium development (in C. albicans) and finally, ceU death. High concentrations of miconazole, which may be achieved with topical use, disturb the orientation of phosphoHpids in the membranes, which produces leaks (13). 

In a recent study, another method for microwave-assisted heterocycle synthesis leading to a small set of imidazole derivatives has been reported [54], These pharmaceutically important scaffolds were synthesized utilizing polymer-bound 3-N,N-(dimethylamino)isocyanoacrylate. This polymer support was easily prepared by treatment of [4-(bromomethyl)phenoxy]methyl polystyrene with a twofold excess of the appropriate isocyanoacrylate potassium salt in N,N-dimethylformamide (Scheme 7.37). The obtained intermediate was subsequently treated with N,N-di-methylformamide diethyl acetal (DMFDEA) in a mixture of tetrahydrofuran and ethanol to generate the desired polymer-bound substrate. 

Derivatives of bzacen have been studied to a minor extent [Fe(bzacen) (N-methyl-imidazole)2]C104 [176] and [Fe(bzacen)(Him)(CN)] [185] are purely low spin, whereas [Fe(bzacen)(Him)2]BPh4 shows gradual spin crossover [185]. 

An intramolecular heteroaryl Heck was the pivotal step in the synthesis of 5-butyl-1-methyl-l//-imidazo[4,5-c]quinolin-4(5//)-one (63), a potent antiasthmatic agent [46], The optimum yield was obtained under Jeffery s ligand-free conditions, echoing Ohta s observation for the intermolecular version. Once again, the Caryi—Caryi bond was constructed at the C(5) position of the imidazole ring. Another intramolecular heteroaryl Heck cyclization of pyrrole and imidazole derivatives was also reported to assemble annulated isoindoles [47]. 

A comparison of the S-methylation of a trimethyltriazolinethione with a similar imidazole derivative suggested a later transition state for the triazolinethione <83JCS(P2)1217>. 

Aus l-[(2-Trimethylsilyl-ethoxy)-methyl]-imidazol konnen in Eintopfsynthesen durch sukzessive Metallierung und Umsetzung mit Elektrophilen 1,2,5-trisubstituierte Derivate wie z. B. 5-Formyl-2-phenylthio-1 -[2- (trimethylsilyl-ethoxy) -methyl]- (90%) oder 2-Phenylthio-1-[2-(trimethylsilyl-ethoxy)-methyl]-5-trimethylsiloxy-imidazol (79%) hergestellt werden1024. 

H3 Receptor Agonist Activity of Imidazole-methylated Histamine Derivatives... 

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