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Mono-N-alkylation of Amphotericin B and Nystatin A₁ and Its Amides: Effect on the In Vitro Activity, Cytotoxicity and Permeabilization of Model Membranes.

ABSTRACT: Objectives: In 2022, the World Health Organization highlighted the necessity for the development of new antifungal agents. Polyene antibiotics are characterized by a low risk of drug resistance; however, their use is limited by low solubility and severe side effects. Methods: A series of N-alkylated derivatives of amphotericin B and nystatin A₁ as well as their N-(2-hydroxyethyl)amides were synthesized. Their antifungal activity was evaluated against various Candida strains and Aspergillus fumigatus using the broth microdilution method. Cytotoxicity was assessed using an MTT assay on human embryonic kidney cells HEK293 and human skin fibroblast cells hFB-hTERT6, as well as a hemolysis assay on erythrocytes. Membrane activity was analyzed

SUBMITTER: Omelchuk O

PROVIDER: S-EPMC11672593 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature

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Mono-N-alkylation of Amphotericin B and Nystatin A₁ and Its Amides: Effect on the In Vitro Activity, Cytotoxicity and Permeabilization of Model Membranes.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Mono-N-alkylation of Amphotericin B and Nystatin A1 and Its Amides: Effect on the In Vitro Activity, Cytotoxicity and Permeabilization of Model Membranes.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Mono-N-alkylation of Amphotericin B and Nystatin A₁ and Its Amides: Effect on the In Vitro Activity, Cytotoxicity and Permeabilization of Model Membranes.