ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans

The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substan...

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Detalles Bibliográficos
Autores principales: Youngsaye, Willmen, Hartland, Cathy L, Morgan, Barbara J, Ting, Amal, Nag, Partha P, Vincent, Benjamin, Mosher, Carrie A, Bittker, Joshua A, Dandapani, Sivaraman, Palmer, Michelle, Whitesell, Luke, Lindquist, Susan, Schreiber, Stuart L, Munoz, Benito
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Beilstein-Institut 2013
Materias:
Full Research Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3740683/
https://www.ncbi.nlm.nih.gov/pubmed/23946849
http://dx.doi.org/10.3762/bjoc.9.171
Descripción
Sumario:The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure–activity relationships led to the discovery of ML212.

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