Structure鈥揂ctivity Relationships among Antifungal Nylon-3 Polymers: Identification of Materials Active against Drug-Resistant Strains of Candida albicans

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• 作者：Runhui Liu ; Xinyu Chen ; Shaun P. Falk ; Brendan P. Mowery ; Amy J. Karlsson ; Bernard Weisblum ; Sean P. Palecek ; Kristyn S. Masters ; Samuel H. Gellman
• 刊名：Journal of the American Chemical Society
• 出版年：2014
• 出版时间：March 19, 2014
• 年：2014
• 卷：136
• 期：11
• 页码：4333-4342
• 全文大小：524K
• 年卷期：v.136,no.11(March 19, 2014)
• ISSN：1520-5126

文摘

Fungal infections are a major challenge to human health that is heightened by pathogen resistance to current therapeutic agents. Previously, we were inspired by host-defense peptides to develop nylon-3 polymers (poly-尾-peptides) that are toxic toward the fungal pathogen Candida albicans but exert little effect on mammalian cells. Based on subsequent analysis of structure鈥揳ctivity relationships among antifungal nylon-3 polymers, we have now identified readily prepared cationic homopolymers active against strains of C. albicans that are resistant to the antifungal drugs fluconazole and amphotericin B. These nylon-3 polymers are nonhemolytic. In addition, we have identified cationic鈥揾ydrophobic copolymers that are highly active against a second fungal pathogen, Cryptococcus neoformans, and moderately active against a third pathogen, Aspergillus fumigatus.