The three imidazole antimycotics clotrimazole, miconazole, and ketoconazole all inhibit the demethylation of lanosterol to ergosterol, resulting in inhibition of growth of Saccharomyces cerevisiae; this is a fungistatic action. At higher concentrations clotrimazole and miconazole are fungicidal, whereas ketoconazole is not. The fungicidal action reflects direct membrane damage by the imidazoles...

A short and efficient synthesis of 1,4-disubstituted imidazoles has been developed which provides the desired products with complete regioselectivity. This protocol allows preparation of compounds which are challenging to prepare by current literature methods in a regioselective fashion, a sterically and electronically diverse range of N-substituents being accessible. The sequence involves an u...

2-Imidazolines and imidazoles have been accessed by an aza-Wittig sequence featuring novel N-acylation methodology for sulfonamides and optimized conditions for ring closure.

Nickel(0) catalysts were used to produce substituted imidazoles in good to high yields using benzonitrile, p-substituted benzonitriles and 4-cyanopyridine as starting materials.

N-Glucuronidation in vitro of six 4-arylalkyl-1H-imidazoles (both enantiomers of medetomidine, detomidine, atipamezole, and two other closely related compounds) by rat, dog, and human liver microsomes and by four expressed human UDP-glucuronosyltransferase isoenzymes was studied. Human liver microsomes formed N-glucuronides of 4-arylalkyl-1H-imidazoles with high activity, with apparent V(max) v...

Urocanic acid (UCA) derivatives were tested for their anti-inflammatory activity in inflammatory bowel disease (IBD) in two models: ex vivo and an experimental mouse model. Ex vivo: inflamed colonic tissue was incubated in culture medium with or without the UCA derivatives. Biopsies, incubated with UCA derivatives, produced lower levels of proinflammatory cytokines IL-6 and IL-8 as compared to ...

A catalytic method involving carbenoid insertion onto dihydroimidazoles is reported for the generation of dihydroimidazolium ylides, and their subsequent diastereoselective cycloaddition to form pyrrolo[1,2-a]imidazoles © 2009 Elsevier Science. All rights reserved ———

A novel and straightforward synthetic protocol for the efficient construction of 3',5'-dihydro-1H-spiro[benzo[d]oxepine-2,4'-imidazoles] through a copper(I)-catalyzed reaction between 2-(2-ethynylphenyl)oxirane, sulfonyl azide, and 2-isocyanoacetate is described.