Structure–Activity Relationships among Antifungal Nylon-3 Polymers: Identification of Materials Active against Drug-Resistant Strains of Candida albicans | Zendy

Runhui Liu | Zendy; Xinyu Chen | Zendy; Shaun P. Falk | Zendy; Brendan P. Mowery | Zendy; Amy J. Karlsson | Zendy; Bernard Weisblum | Zendy; Sean P. Palecek | Zendy; Kristyn S. Masters | Zendy; Samuel H. Gellman | Zendy

Open Access

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

Author(s) -

Runhui Liu,

Xinyu Chen,

Shaun P. Falk,

Brendan P. Mowery,

Amy J. Karlsson,

Bernard Weisblum,

Sean P. Palecek,

Kristyn S. Masters,

Samuel H. Gellman

Publication year - 2014

Publication title -

journal of the american chemical society

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 7.115

H-Index - 612

eISSN - 1520-5126

pISSN - 0002-7863

DOI - 10.1021/ja500036r

Subject(s) - candida albicans , pathogen , cryptococcus neoformans , aspergillus fumigatus , microbiology and biotechnology , chemistry , fungal pathogen , fluconazole , antifungal drug , corpus albicans , cationic polymerization , amphotericin b , antifungal , human pathogen , biochemistry , biology , organic chemistry , gene

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-β-peptides) that are toxic toward the fungal pathogen Candida albicans but exert little effect on mammalian cells. Based on subsequent analysis of structure-activity 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-hydrophobic copolymers that are highly active against a second fungal pathogen, Cryptococcus neoformans, and moderately active against a third pathogen, Aspergillus fumigatus.

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