Flavohemoglobins metabolize nitric oxide (NO) to nitrate and protect bacteria and fungi from NO-mediated damage, growth inhibition, and killing by NO-releasing immune cells. Antimicrobial imidazoles were tested for their ability to coordinate flavohemoglobin and inhibit its NO dioxygenase (NOD) function. Miconazole, econazole, clotrimazole, and ketoconazole inhibited the NOD activity of Escheri...

DURING A STUDY on the metabolism of histidine in a child affected with histidinemia (Beauvais, P., and Humbel, R., to be published), we became interested in the chromatography of imidazoles. In this disease the urine contains numerous imidazoles: histidine and its metabolites, imidazole-pyruvic, imidazole-lactic and imidazole-acetic acids and N-acetylhistidine.’I developed a chromatographic met...

Disubstituted imidazoles were prepared by reacting appropriate phenylglyoxal with different aryl aldehydes in the presence of ammonium acetate. Trisubstituted imidazoles were prepared by reacting disubstituted imidazoles with chlorobenzene in the presence of catalytic amount of triethylamine (TEA). The synthesized compounds were characterized on the basis of IR, 1H-NMR and mass spectral data an...

BACKGROUND Azaheterocycles are an important class of compounds because of their highly potent medicinal activities, and the imidazole subcategory is of special interest in regard to drug discovery research. FINDINGS An expeditious synthetic protocol of 2-aryl-4-phenyl-1H-imidazoles has been accomplished by reacting phenylglyoxal monohydrate, ammonium acetate, and aldehyde under sonication. Fo...

A diastereoselective and enantioselective construction of 2,3-disubstituted 1,4-dicarbonyl compounds is reported. Nishiyama's RuPhebox complex (2.0 mol% catalyst loading) serves as a chiral Lewis acid in conjunction with BrCCl3 base for the oxidative homocoupling 2-acyl imidazoles via stereocontrolled reaction intermediate Ru enolates situ brominated imidazoles. Cleavage achiral imidazole auxil...

The completely N1-selective Pd-catalyzed arylation of unsymmetric imidazoles with aryl halides and triflates is described. This study showed that imidazoles have a strong inhibitory effect on the in situ formation of catalytically-active Pd(0)-ligand complex. The efficacy of the N-arylation reaction was improved drastically by the use of pre-activated solution of Pd2(dba)3 and L1. From these fi...

Substituted imidazoles are of interest because their useful biological activities. While several methods have been developed for the synthesis such compounds, some reported utilize corrosive or toxic catalysts. We report a bismuth (III) triflate catalyzed multicomponent 2,4,5-trisubstituted imidazoles. Bismuth compounds attractive from green chemistry perspective they remarkably non-toxic and n...

Di & tri substituted imidazoles were prepared by condensing phenylglyoxal with different aryl aldehydes in presence of ammonium acetate and glacial acetic acid. All the di and tri substituted imidazoles were characterized by spectral analysis i.e. HNMR and Mass spectral data. All the synthetic compounds were screened for there anti-inflammatory and anti bacterial activity.

The reaction of protected 4,5-diiodoimidazoles with (PhMe2CCH2)2CuLi regioselectively provides 5-cuprated imidazoles, which readily react with various electrophiles furnishing functionalized imidazoles in good yields; remarkably, these resulting mono-iodoimidazoles undergo again an iodine-copper exchange reaction in the presence of sensitive functional groups, like an aldehyde or a ketone.

Imidazoles and triazoles represent major classes of antifungal azole derivatives. With respect to UDP-glucuronosyltransferase (UGT) enzymes, the drug metabolism focus has mainly concentrated on their inhibitory effects with little known about azoles as substrates for UGTs. N-Glucuronide metabolites of the imidazole antifungals, tioconazole and croconazole, have been reported, but there are curr...