DOI: 10.1128/aac.42.10.2495. Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents

Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents

10.1128/aac.42.10.2495

Crossref journal-article

American Society for Microbiology

Antimicrobial Agents and Chemotherapy (235)

Abstract

ABSTRACT Twenty analogues of pentamidine, 7 primary metabolites of pentamidine, and 30 dicationic substituted bis-benzimidazoles were screened for their inhibitory and fungicidal activities against Candida albicans and Cryptococcus neoformans . A majority of the compounds had MICs at which 80% of the strains were inhibited (MIC 80 s) comparable to those of amphotericin B and fluconazole. Unlike fluconazole, many of these compounds were found to have potent fungicidal activity. The most potent compound against C. albicans had an MIC 80 of ≤0.09 μg/ml, and the most potent compound against C. neoformans had an MIC 80 of 0.19 μg/ml. Selected compounds were also found to be active against Aspergillus fumigatus , Fusarium solani , Candida species other than C. albicans , and fluconazole-resistant strains of C. albicans and C. neoformans . It is clear from the data presented here that further studies on the structure-activity relationships, mechanisms of action and toxicities, and in vivo efficacies of these compounds are warranted to determine their clinical potential.

Bibliography

Del Poeta, M., Schell, W. A., Dykstra, C. C., Jones, S., Tidwell, R. R., Czarny, A., Bajic, M., Bajic, M., Kumar, A., Boykin, D., & Perfect, J. R. (1998). Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents. Antimicrobial Agents and Chemotherapy, 42(10), 2495â2502.

Authors 11

Maurizio Del Poeta (first)
Wiley A. Schell (additional)
Christine C. Dykstra (additional)
Susan Jones (additional)
Richard R. Tidwell (additional)
Agnieszka Czarny (additional)
Miroslav Bajic (additional)
Marina Bajic (additional)
Arvind Kumar (additional)
David Boykin (additional)
John R. Perfect (additional)

References 41 Referenced 203

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Berger B. J. Reddy V. V. Le S. T. Lombardy R. J. Hall J. E. Tidwell R. R. Hydroxylation of pentamidine by rat liver microsomes. J. Pharmacol. Exp. Ther. 256 1991 883 889 / J. Pharmacol. Exp. Ther. / Hydroxylation of pentamidine by rat liver microsomes. by Berger B. J. (1991)
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Dates

Type	When
Created	6 years, 10 months ago (Oct. 8, 2018, 8:29 p.m.)
Deposited	3 years, 6 months ago (Feb. 21, 2022, 10:42 a.m.)
Indexed	26 minutes ago (Aug. 26, 2025, 11:38 p.m.)
Issued	26 years, 10 months ago (Oct. 1, 1998)
Published	26 years, 10 months ago (Oct. 1, 1998)
Published Print	26 years, 10 months ago (Oct. 1, 1998)

Funders 0

None

BibTeX

@article{Del_Poeta_1998, title={Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents}, volume={42}, ISSN={1098-6596}, url={http://dx.doi.org/10.1128/aac.42.10.2495}, DOI={10.1128/aac.42.10.2495}, number={10}, journal={Antimicrobial Agents and Chemotherapy}, publisher={American Society for Microbiology}, author={Del Poeta, Maurizio and Schell, Wiley A. and Dykstra, Christine C. and Jones, Susan and Tidwell, Richard R. and Czarny, Agnieszka and Bajic, Miroslav and Bajic, Marina and Kumar, Arvind and Boykin, David and Perfect, John R.}, year={1998}, month=oct, pages={2495–2502} }

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      "group": {
        "name": "publication_history",
        "label": "Publication History"
      }
    },
    {
      "value": "1998-10-01",
      "order": 2,
      "name": "published",
      "label": "Published",
      "group": {
        "name": "publication_history",
        "label": "Publication History"
      }
    }
  ]
}