Disease relevance of BENZIMIDAZOLE

• Flubendazole, an injectable benzimidazole drug, was compared with diethylcarbamazine (DEC) in a prospective double-blind study of the treatment of onchocerciasis [1].
• With the discovery of several new types of inotropic agents, i.e., the bipyridines and the imidazole and benzimidazole derivatives, interest in revising our therapeutic approach to congestive heart failure has increased [2].
• Substantial amounts of an additional protein of molecular weight 38,000 (38K) become cross-linked to the mRNA when cells are treated with inhibitors of mRNA synthesis (actinomycin D, camptothecin, and 5,6-dichloro-1-beta-D-ribofuranosyl benzimidazole) or after infection with vesicular stomatitis virus [3].
• Clinical trials of omeprazole, a substituted benzimidazole, indicate that it is safe and effective for short-term treatment of patients with duodenal or gastric ulcer, and it is highly effective for long-term treatment of patients with Zollinger-Ellison syndrome [4].
• Liarozole fumarate (R85,246), a novel benzimidazole derivative, reduced s.c. and bone metastasis tumor growth by the androgen-independent PC-3ML-B2 human prostatic carcinoma clone in SCID mice [5].
• This has major implications for parasite control programs dependent on MLs/benzimidazole rotations and on the use of ML/benzimidazole combination therapy, such as for human lymphatic filariasis and nematode control in ruminant livestock [6].

Psychiatry related information on BENZIMIDAZOLE

• Quinoline and benzimidazole derivatives: candidate probes for in vivo imaging of tau pathology in Alzheimer's disease [7].

High impact information on BENZIMIDAZOLE

• The mad (mitotic arrest-deficient) and bub (budding uninhibited by benzimidazole) mutants of budding yeast lack this checkpoint and fail to arrest the cell cycle when microtubules are depolymerized [8].
• The concentrations of the benzimidazole ribosides at which the rate of proliferation of human fibroblasts (FS-4) is reduced by 50% are as follows: monobromodichloro: 1.7 muM (0.68 mug/ml); dibromo: 12 muM (4.9 mug/ml); dichloro: 38 muM (12 mug/ml) [9].
• A comparative study of the effects of certain halogenated benzimidazole ribosides on RNA synthesis, cell proliferation, and interferon production [9].
• This substituted benzimidazole molecule had been shown to decrease several liver cytochrome P450-mediated monooxygenase activities both in vitro and in vivo [10].
• Effects of substituted benzimidazole (H 149/94) on gastric acid secretion in humans [11].

Chemical compound and disease context of BENZIMIDAZOLE

• Resistance of human cytomegalovirus to the benzimidazole L-ribonucleoside maribavir maps to UL27 [12].
• Albendazole (ABZ) is a benzimidazole anthelmintic drug used in the treatment of neurocysticercosis [13].
• Drugs such as tomeglovir (BAY-384766), 2-bromo-5,6-dichloro-1beta-D-ribofuranosyl benzimidazole (BDCRB) and GW-275175X act as inhibitors of the terminase complex that is involved in cleavage and packaging of the unit length DNA into the capsids [14].
• The narrow binding pocket allows a maximum torsion angle between the phenyl and benzimidazole rings of about 40 degrees, consistent with that calculated (43.6 degrees) for the minimum-energy conformation of the unsubstituted free ligand [15].
• Mechanism of action of the ribopyranoside benzimidazole GW275175X against human cytomegalovirus [16].

Biological context of BENZIMIDAZOLE

• The kinetics of benzimidazole dissociation in methylcobalamin [17].
• DNA sequence dependent monomer-dimer binding modulation of asymmetric benzimidazole derivatives [18].
• The benzimidazole subunits of the ligand participate in six bifurcated hydrogen bonds with A:T base pair edges, three to each DNA strand [19].
• Resistance which maps to two different genes suggests that their putative proteins interact and/or that either or both have a benzimidazole ribonucleoside binding site [20].
• S6 phosphorylation accompanies recruitment of ribosomes and mRNA into polysomes in response to dichlororibofuranosyl benzimidazole [21].

Anatomical context of BENZIMIDAZOLE

• AR-L 115BS, a benzimidazole derivative, is a positive inotropic agent that has been shown to increase active tension development and unloaded shortening velocity of chemically skinned heart muscle preparations at submaximal activating levels of free Ca++ [22].
• Pharmacokinetic disposition of benzimidazole drugs in the ruminant gastrointestinal tract [23].
• The lack of cross-resistance of the NocR and Podrii6 cell lines to thiabendazole provides evidence that the mechanism of action of this compound is different from that of other benzimidazole carbamate derivatives [24].
• Isolated rat liver cells were pulse-labelled with tritiated uridine and post-incubated in the presence of an excess of unlabelled uridine and of adenosine analog DRB (5-6-dichloro-1-beta-D-ribofuranosyl benzimidazole) [25].
• A highly specific benzimidazole pyridazinone reverses phosphate-induced changes in cardiac myofilament activation [26].

Associations of BENZIMIDAZOLE with other chemical compounds

• To demonstrate therapeutic efficacy in vivo, hamsters infected with A. ceylanicum were treated with three daily oral doses of purified Cry5B, the benzimidazole anthelminthic mebendazole, or buffer [27].
• In this report, we describe an unusual example of a structural rearrangement near a buried artificial cavity in cytochrome c peroxidase that occurs on binding protonated benzimidazole [28].
• Our clinical trial with albendazole, one of the benzimidazole carbamates, has included 26 cases of AE since September 1988, each of whom had undergone an operation [29].
• The kinetically obtained pKa values of 6.94 +/- 0.02, 6.93 +/- 0.03, and 5.60 +/- 0.05 for imidazole, methylimidazole, and benzimidazole, respectively, match the values obtained by titrimetric pKa determination, indicating the requirement for an unprotonated nitrogen for binding to QC [30].
• The usefulness of parbendazole and other benzimidazole carbamates as inhibitors of microtubule functions is discussed [31].

Gene context of BENZIMIDAZOLE

• Components of the spindle checkpoint include the mitotic arrest defective (MAD) genes MAD1-3, and the budding uninhibited by benzimidazole (BUB) genes BUB1 and BUB3 [32].
• Cell division cycle genes nda2 and nda3 of the fission yeast Schizosaccharomyces pombe control microtubular organization and sensitivity to anti-mitotic benzimidazole compounds [33].
• IGF-I and RA did not change IGFBP-5 mRNA stability in Ob cells after transcription arrest with the RNA polymerase II inhibitor 5,6-dichloro-1-beta-D-ribofuranosyl benzimidazole [34].
• Site-directed mutagenesis of Saccharomyces cerevisiae beta-tubulin: interaction between residue 167 and benzimidazole compounds [35].
• Benzimidazole derivatives. 4. The recognition of the voluminous substituent attached to the basic amino group of 5-HT4 receptor antagonists [36].

Analytical, diagnostic and therapeutic context of BENZIMIDAZOLE

• Conformation of nucleosides: circular dichroism study on the syn-anti conformational equilibrium of 2-substituted benzimidazole nucleosides [37].
• Combinations that include the benzimidazole 5-carboxamide polymerase inhibitors and compounds that bind other sites or other HCV targets, including HCV protease inhibitors, are complementary in cell culture models of HCV RNA replication at suppressing the emergence of resistant variants [38].
• Use of benzimidazole chemotherapy in human helminthiases: indications and efficacy [39].
• Although benzimidazole derivatives such as mebendazole and albendazole are being used as therapeutic agents, there is often no complete recovery after treatment [40].
• Activities of benzimidazole D- and L-ribonucleosides in animal models of cytomegalovirus infections [41].

References