In vitro screening of pentamidine analogs against bacterial and fungal strains

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• 作者：Dorota Maciejewska^a ; ^{dmaciejewska@wum.edu.pl" class="auth_mail} ; Jerzy 呕abi艅ski^a ; Pawe艂 Ka藕mierczak^a ; Karolina Wó ; jciuk^b ; Marcin Kruszewski^b ; ^c ; Hanna Kruszewska^d ; ^&dagger ;
• 关键词：Linear pentamidine analogs ; Anti-bacterial activity ; Anti-fungal activity ; Anti-MRSA activity ; Structure&ndash ; activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 July 2014
• 年：2014
• 卷：24
• 期：13
• 页码：2918-2923
• 全文大小：483 K

文摘

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.