Carboxylesterases are among the best characterized prodrug-hydrolyzing enzymes involved in the activation of several therapeutic carbamate and ester prodrugs. The broad specificity of these enzymes makes them amenable for designing prodrugs. Porcine liver carboxylesterase 1 specificity for amino acid esters of three nucleoside analogs [floxuridine, gemcitabine, and 2-bromo-5,6-dichloro-1-(beta-...

The stability constants of species present in the systems Ni(II)-pyridoxamine(pym)(A) and Ni(II)-pyridoxamine(pym)(A)-imidazole containing ligands(B) [B = imidazole(him),  benzimidazole(bim), histamine(hist) and L-histidine(his)] have been determined pH-metrically using the MINIQUAD computer program. The existence of the species NiAH, NiA and NiA2 was proven for the Ni(II)-pym(A)...

Herein, we report a bulky variant of bis-benzimidazole carboxylate ligand. The five-position the benzimidazole groups were substituted with tertiary butyl intention preventing bis-ligation and oligomerization, as was observed in other studies using similar ligands. Unfortunately, even bulkier substituents, new ligand still formed bis-ligated structure. Although did not afford desired mono-ligat...

Benzimidazole, which is a heterocyclic nucleus, plays an important role in various medicines. A number of therapeutic agents such as H1 antihistaminic agent clemizole, a potent opioid analgesic etonitazene, nonnucleoside antiviral compound enviroxime, for promotion of excretion of uric acid irtemazole, non sedating antihistaminic agent astemizole, anti ulcer drugs omeprazole and pentoprazole, a...

The spin transition temperatures of [Fe(didentate)3]2+in acetonitrile (didentate = 2-X-benzimidazole) can be stepwise decreased by 40 K along the series X pyrazine > pyridine pyrimidine.

The cation of the title compound, C(14)H(14)N(3) (+)·I(-), is non-planar, the dihedral angle between the benzimidazole and the 1-methyl-pyridinium planes being 37.4 (2)°. The crystal structure is stabilized by weak π-π stacking inter-actions, the centroid-centroid distances between 1-methyl-imidazole and benzimidazole planes being 3.678 (4) Å.

The title mol-ecule, C(25)H(26)N(2)Se, has mirror symmetry, with the mirror plane passing through the atoms of the C=Se bond and the mid-points of the two C-C bonds of the benzene ring of the benzimidazole group. The dihedral angle between the benzimidazole ring system and the phenyl ring is 71.62 (14)°.

The design and synthesis of a series of methyl 5(6)-substituted benzimidazole-2-carbamates as possible anthelmintics have been described. A rational analysis of the structural parameters which segregate the activity of resulting benzimidazole-2-carbamates against enteric and tissue dwelling helminths is presented. The influence of single and multiple spacers, which link the pharmacophores at 5(...

A series of 22 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5- carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activity against S. aureus and methicillin resistant S. aureus (MRSA), E. coli, E. faecalis and for antifungal activity against C. albicans. Compound 59 [1-(2,4-dichlorobenzyl)-N- (2-diethylaminoethyl)-1H-benzimidazole-5-carboxamidine], with ...

Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia...