Saber UCV
Repositorio Institucional
Repositorio Institucional
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https://saber.ucv.ve/handle/10872/302
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| Title: | Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents |
| Authors: | Camacho, José Barazarte, Arthur Gamboa, Neira Rodrigues, Juan Rojas, Rosario Vaisberg, Abraham Gilman, Robert Charris, Jaime |
| Keywords: | Antimalarial Benzimidazole Plasmodium berghei b-Hematin Tuberculosis Cancer |
| Issue Date: | 1-Feb-2011 |
| Publisher: | Bioorganic & Medicinal Chemistry |
| Abstract: | A series of N0-substituted-2-(5-nitrofuran or 5-nitrothiophen-2-yl)-3H-benzo[d]imidazole-5-carbohydrazide derivatives were synthesized and investigated for their abilities to inhibit b-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei. Selected analogues were screened for their antitubercular activity against sensitive MTB H37Rv and multidrugresistant MDR-MTB strains, and cytotoxic activity against a panel of human tumor cell lines and two nontumourogenic cell lines. Compounds 3a, 5a, f, 6g were the most promising as inhibitors of b-hematin formation, however, their effect as inhibitors of hemoglobin hydrolysis were marginal. The most active compounds to emerge from the in vitro and in vivo murine studies were 3a and 6i, suggesting an antimalarial activity via inhibition of b-hematin formation and are as efficient as chloroquine. The cytotoxic and antitubercular activities of the present compounds were not comparable with those of the standard drugs employed. But, however, compound 5b showed better antitubercular activity compared to rifampin against multidrug-resistant MDR-MTB strains. Compounds 3a, 6i and 5b showed a good safety index |
| URI: | http://hdl.handle.net/10872/302 |
| Appears in Collections: | Artículos Publicados |
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