In vitro screening of pentamidine analogs against bacterial and fungal strains |
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| Institution: | 1. Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Banacha 1, 02-097 Warsaw, Poland;2. Department of Inorganic and Analytical Chemistry, University of Szeged, Dóm tér 7, H-6720 Szeged, Hungary;1. Department of Biological Sciences, College of Biological Science and Biotechnology, Konkuk University, Seoul 143-701, Republic of Korea;2. Cancer and Metabolism Institute, Konkuk University, Seoul 143-701, Republic of Korea;3. Division of Bioscience and Biotechnology, BMIC, Konkuk University, Seoul 143-701, Republic of Korea |
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| 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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| Keywords: | Linear pentamidine analogs Anti-bacterial activity Anti-fungal activity Anti-MRSA activity Structure–activity |
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