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  • 1
    Digitale Medien
    Digitale Medien
    Structure and conformation of dihydro aromatic compounds. 3. Cis- and trans-disubstituted 1,4-dihydrobenzenes, 1,4-dihydronaphthalenes, and 9,10-dihydroanthracenes (1984)
    s.l. : American Chemical Society
    Journal of the American Chemical Society 106 (1984), S. 3119-3123 
    Details
    ISSN: 1520-5126
    Quelle: ACS Legacy Archives
    Thema: Chemie und Pharmazie
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1021/ja00323a008
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  • 2
    Digitale Medien
    Digitale Medien
    Efficacy of albendazole and mebendazole againstHymenolepis microstoma andHymenolepis diminuta (1992)
    Springer
    Parasitology research 78 (1992), S. 108-111 
    Details
    ISSN: 1432-1955
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract An investigation of the chemotherapeutic effects of 2 anthelmintics, albendazole (ABZ, methyl 5-[propylthio]benzimidazole-2-carbamate) and mebendazole (MBZ, methyl 5-[benzoyl]benzimidazole-2-carbamate), onHymenolepis microstoma andHymenolepis diminuta in experimentally infected mice and rats is reported. Single (50 mg/kg) or multiple daily oral doses (50 mg kg−1 day−1 for 3 consecutive days) of MBZ had no effect onH. microstoma; at necropsy, the drug treated mice harbored appreciable numbers of the parasite in the bile duct and biliary passages. ABZ was also inactive when given as a single oral 50 mg/kg dose on day 27 PI. Better results were obtained when ABZ was administered at a dosage of 50 mg kg−1 day−1 for 3 consecutive days; the reduction in worm burden obtained with this treatment regimen was 50%. These results are in marked contrast to those obtained with the same anthelmintics against enteralH. diminuta in rats which succumbed at lower dosages. A review was made of the published reports on the pharmacokinetic behavior of these benzimidazole carbamate anthelmintics and a hypothesis for the inactivity of MBZ againstH. microstoma is proposed.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00931650
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  • 3
    Digitale Medien
    Digitale Medien
    Molecular modeling: a tool for predicting anthelmintic activity in vivo (1993)
    Springer
    Parasitology research 79 (1993), S. 475-479 
    Details
    ISSN: 1432-1955
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Abstract The structural and electronic features of the broad-spectrum benzimidazole anthelmintic mebendazole [MBZ, methyl 5-(benzoyl)-benzimidazole-2-carbamate] have been determined using a combination of quantum mechanics, molecular graphics, and molecular modeling techniques. Using conformational analyses and quantum mechanics, we found that the three-dimensional structure and electronic features of MBZ were consistent with those previously reported for highly active broad-spectrum benzimidazole anthelmintics and that in vivo drug efficacy againstHymenolepis diminuta depends upon the orientation of the benzoyl group at position 5 on the heterocyclic ring system, the magnitude of the molecular dipole moment, and the percentage of polar surface area. The chemotherapeutic actions of MBZ onH. diminuta in vivo were accompanied by marked changes in worm weight and chemical composition. Tapeworms recovered from rats that had received a therapeutically effective dose of MBZ 24 h earlier were significantly smaller and contained much less glycogen (as a percentage of the wet weight) than worms from untreated controls. In MBZ-treated worms, protein concentrations rose at a rate sufficient to offset the decline in glycogen concentration. Glycogen/protein ratios in MBZ-treated worms were considerably lower than the corresponding control values. Differences in the absolute amounts of glycogen between control and drug-treated worms were even more profound. Administration of a curative dose of MBZ to the rat host produced inH. diminuta another change, the onset of which coincided with the gross alterations in worm weight and chemical composition. In vitro studies carried out 24 h after treatment revealed that MBZ-treated worms absorbed and metabolized much smaller quantities of exogenous glucose than did the controls and that the ability of the worm to accumulate glucose against a concentration difference was significantly depressed. A mode of action common to MBZ and other structurally related broad-spectrum benzimidazole anthelmintics is further indicated by the similarity of their biochemical and physiological effects on the tapeworms and their time course of action following their administration to rats infected withH. diminuta.
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1007/BF00931586
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  • 4
    Digitale Medien
    Digitale Medien
    Announcement (1982)
    New York, NY : Wiley-Blackwell
    International Journal of Quantum Chemistry 22 (1982), S. 1307-1307 
    Details
    ISSN: 0020-7608
    Schlagwort(e): Computational Chemistry and Molecular Modeling ; Atomic, Molecular and Optical Physics
    Quelle: Wiley InterScience Backfile Collection 1832-2000
    Thema: Chemie und Pharmazie
    Materialart: Digitale Medien
    URL: http://dx.doi.org/10.1002/qua.560220612
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