This is a study of a small group of patients with rheumatoid arthritis, in whom the urine excretion of imidazole compounds was examined by Figlu assay and chromatography of 12-hour urine collections following 15 g. histidine load, and by assay of 4 amino-imidazole-5 carboxamide (AIC) in 12hour urines with and without histidine load. Gough, McCarthy, Read, Mollin, and Waters (1964) found low ser...

Resonance Raman spectroscopy has been used to observe changes in the iron-ligand stretching frequency in photoproduct spectra of the proximal cavity mutant of myoglobin H93G. The measurements compare the deoxy ferrous state of the heme iron in H93G(L), where L is an exogenous imidazole ligand bound in the proximal cavity, to the photolyzed intermediate of H93G(L)*CO at 8 ns. There are significa...

Misonidazole, after reduction to the hydroxylamine deriva tive, was found to react with guanosine in aqueous solution at pH 7. The guanosine product was isolated and was assigned a structure having a new 5-membered ring with a —CHOHCHOH-linkage between the N-1 and N-2 positions of guanine. Removal of the sugar residue from the guanosine product by acid hydrolysis resulted in the corresponding...

A series of eight 1-substituted imidazoles was investigated as model substrates for glucuronidation at an aromatic tertiary amine of polyaza heterocyclic ring systems. The human UDP-glucuronosyltransferases (UGTs) involved and substrate specificities were investigated. Nine expressed enzymes (UGT1A1, UGT1A3, UGT1A4, UGT1A6, UGT1A7, UGT1A9, UGT1A10, UGT2B7, and UGT2B15) were examined, but only U...

Rhodococcus equi and species of Nocardia and Gordonia may be human opportunistic pathogens. We find that these, as well as several isolates from closely related genera, are highly susceptible to the imidazoles bifonazole, clotrimazole, econazole, and miconazole, whose MICs are </=1 micro g/ml. In liquid cultures 1 micro g of the drug/ml was bacteriostatic and 10 micro g/ml was bactericidal. On ...

Fe(3)O(4) nanoparticles were prepared by chemical coprecipitation method and subsequently coated with 3-aminopropyltriethoxysilane (APTES) via silanization reaction. Grafting of chlorosulfuric acid on the amino-functionalized Fe(3)O(4) nanoparticles afforded sulfamic acid-functionalized magnetic nanoparticles (SA-MNPs). SA-MNPs was found to be a mild and effective solid acid catalyst for the ef...

A series of 1,2,4-trisubstituted-1H- imidazole derivatives (4a-o) was synthesized by reacting 2,4-disubstituted-1H-imidazoles (3a-o) with chlorobenzene in the presence of triethylamine. Phenylglyoxal (2) was reacted with different aromatic aldehydes in the presence of ammonium acetate and glacial acetic acid to afford the disubstituted imidazoles (3a-o). The structures of the synthesized compou...

the highly substituted pyridine derivatives are found to exhibit diverse pharmacological activities. they are also emerged as potential medicinal leads in developing therapeutic agents for the treatment of various diseases. in this work, a series of 2-amino-3,5-dicarbonitrile-6-thio-pyridine derivatives have been synthesized at room temperature via one-pot, multi-component reaction of various a...

The synthesis of trifluoromethyl-substituted pyridylboronic acids and pyrazolylboronic esters is described via lithiation-boronation protocols (Schemes 1, 3 and 4). A study of their palladium-catalysed cross-couplings with heteroaryl halides is presented. CF3-substituted aryl/heteroaryl-pyridines are thereby obtained (51-98% yields). Analogous cross-couplings have yielded heteroaryl-3-(trifluor...