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Hydroxystilbamidine

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Book cover Mechanism of Action of Antieukaryotic and Antiviral Compounds

Part of the book series: Antibiotics ((1512,volume 5 / 2))

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Abstract

Hydroxystilbamidine (OH.SA.) is hydroxy-4-4′ diamidino stilbene used as diisethionate ; as other diamidine compounds (pentamidine, propamidine, stilbamidine, berenil, etc.), it shows strong activity against bacteria, protozoa, and fungi. It is clinically used in systemic mycosis, mainly North American blastomycosis, visceral leishmaniasis, and secondarily in prophylaxis and treatment of African trypanosomiasis, and in cases of malignancy, e.g., multiple myeloma. Pharmacology of OH.SA. has not been studied in such detail as of stilbamidine (SA); its properties are roughly the same but OH.SA. is experimentally and clinically less toxic than SA. So far no resistances have been extensively described. Its mechanism of action is not known well but recent work has shown in vitro or/and in vivo affinity of OH.SA. for nucleic acids, mainly DNA, and biologic effects such as modifications of the kinetoplast-mitochondrial system of Trypanosoma with alteration of extranuclear circular DNA replication. Mitochondrial DNA affinity of OH.SA. can be shown by cytoplasmic mutations in yeast. OH.SA. is a good nonintercalative chemical instrument for nucleic acids conformation studies.

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Authors
  1. B. Festy
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Editors and Affiliations

  1. Department of the Army, Walter Reed Army Institute of Research, Walter Reed Army Medical Center, Washington, D.C., 20012, USA

    Fred E. Hahn Ph.D.

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Festy, B. (1979). Hydroxystilbamidine. In: Hahn, F.E. (eds) Mechanism of Action of Antieukaryotic and Antiviral Compounds. Antibiotics, vol 5 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-46407-2_10

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  • DOI: https://doi.org/10.1007/978-3-642-46407-2_10

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-642-46409-6

  • Online ISBN: 978-3-642-46407-2

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