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Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents

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dc.contributor.author Camacho, J.
dc.contributor.author Barazarte, A.
dc.contributor.author Gamboa, N.
dc.contributor.author Rodrigues, J.
dc.contributor.author Rojas, R.
dc.contributor.author Vaisberg Wollach, Abraham Jaime
dc.contributor.author Gilman, Robert Hugh
dc.contributor.author Charris, J.
dc.date.accessioned 2022-01-18T19:26:45Z
dc.date.available 2022-01-18T19:26:45Z
dc.date.issued 2011
dc.identifier.uri https://hdl.handle.net/20.500.12866/10841
dc.description.abstract A series of N′-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 β-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 multidrug-resistant 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 β-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 β-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. en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries Bioorganic and Medicinal Chemistry
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Humans en_US
dc.subject In Vitro Study en_US
dc.subject Mice|Malaria en_US
dc.subject Plasmodium en_US
dc.subject Unclassified Drug en_US
dc.subject Chloroquine en_US
dc.subject Drug Efficacy en_US
dc.subject Rifampicin en_US
dc.subject Tuberculosis en_US
dc.subject Antitubercular Agents en_US
dc.title Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.bmc.2011.01.050
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.06
dc.relation.issn 1464-3391


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