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  • Title: In vitro screening of pentamidine analogs against bacterial and fungal strains.
    Author: Maciejewska D, Żabiński J, Kaźmierczak P, Wójciuk K, Kruszewski M, Kruszewska H.
    Journal: Bioorg Med Chem Lett; 2014 Jul 01; 24(13):2918-23. PubMed ID: 24830598.
    Abstract:
    A series of linear pentamidine analogs exhibiting low cytotoxicity, active against Pneumocystis carinii, were evaluated for in vitro activities against bacterial and fungal strains. The majority of the tested bis-amidines exhibited marked activities against Gram-positive strains. In view of the fact that the highest potency was found for 1,5-bis(4-amidinophenoxy)-3-thiapentane dihydrochloride 1j with the S atom in the middle of the aliphatic linker, four new pentamidines bearing S atoms were synthesized and also evaluated against MRSA strains. N,N'-Dialkylated pentamidines with S atoms in the linker are the promising lead structures for antimicrobials development.
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