Synthetic Derivatives of Ciclopirox are Effective Inhibitors of Cryptococcus neoformans.

ABSTRACT: Opportunistic fungal infections caused by Cryptococcus neoformans are a significant source of mortality in immunocompromised patients. They are challenging to treat because of a limited number of antifungal drugs, and novel and more effective anticryptococcal therapies are needed. Ciclopirox olamine, a N-hydroxypyridone, has been in use as an approved therapeutic agent for the treatment of topical fungal infections for more than two decades. It is a fungicide, with broad activity across multiple fungal species. We synthesized 10 N-hydroxypyridone derivatives to develop an initial structure-activity understanding relative to efficacy as a starting point for the development of systemic antifungals. We screened the derivatives for antifungal activity against C. neoform

SUBMITTER: Lin J 

PROVIDER: S-EPMC8015083 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature