Using molecular simplification and hybridization approaches, a series of 2-(benzylthio)-1H-benzo[d]imidazoles was synthesized evaluated as in vitro inhibitors Mycobacterium tuberculosis (M. tuberculosis) growth. Compounds 6p 6z were considered the lead compounds from this molecules, with minimal inhibitory concentration (MIC) values 6.9 3.8 μM against M. H37Rv, respectively. Additionally, leadi...

Nitrogen containing heterocyclic compounds have great utility in synthetic, medicinal and material chemistry. Oxazole, isoxazole, thiazole, imidazole their derivatives gained prominence as they constitute the structural features of many bioactive compounds. In fact, amide functionality represents a privileged scaffold biomolecules drugs. The combination two or more heterocycles linked by into o...

A novel series of compounds, derived from 2,5-functionalized imidazoles, have been synthesized as potential bisubstrate inhibitors of protein farnesyltransferase (FTase) using structure-based design. These compounds have a 1,4-diacid chain and a tripeptide connected by an imidazole ring. The synthetic strategy relies on the functionalization at the C-2 position of the heterocycle with the diaci...

Sensitized photooxidation of imidazoles in aqueous solution and in the presence of inorganic phosphate afforded organic phosphates with yields up to 30%. The major phosphorylated product of oxidation of 2-methylimidazole was isolated and identified as the monophosphate of 4,5-dihydroxy-2-methyl-imidazoline with pKa values of 2.0, 5.2, and 9.8. The compound is energy rich in aqueous solution and...

Zinc ion-induced pyrrole hydrogen ionization from a histidyl residue has recently been suggested as the source of the activity-related deprotonation in carbonic anhydrase (EC 4.2.1.1; carbonate hydro-lyase) occurring at pH 7-8. The results offered to support the hypothesis are shown to be deficient. Examination of the literature reveals no precedent for such a pronounced acidification from pK(a...

N-Alkylation of optically active 1-benzyl-4-phenyl-4,5-dihydroimidazole with active alkyl halides and treatment of the so-formed 4,5-dihydroimidazolium ions with DBU in the presence of a range of electron-deficient alkene dipolarophiles, constitutes a 'one-pot' cascade terminating in a 1,3-dipolar cycloaddition reaction that affords optically active pyrrolo[1,2-a]imidazoles. Three bonds of the ...

A new series of 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d]imidazoles, possessing trimethoxyphenyl pharmacophore, were synthesized to evaluate their biological activities as tubulin inhibitors. Cytotoxic activity of the synthesized compounds 7a-f was assessed against several human cancer cell lines, including MCF-7 (breast cancer cell), HEPG2 (liver hepatocellular cells), A549 (adenocarcinomic hu...