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Beilstein J Org Chem DOI:10.3762/bjoc.9.171

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

Publication TypeJournal Article
Year of Publication2013
AuthorsYoungsaye, W, Hartland, CL, Morgan, BJ, Ting, A, Nag, PP, Vincent, B, Mosher, CA, Bittker, JA, Dandapani, S, Palmer, M, Whitesell, L, Lindquist, S, Schreiber, SL, Munoz, B
JournalBeilstein J Org Chem
Volume9
Pages1501-7
Date Published2013
ISSN1860-5397
Abstract

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.

DOI10.3762/bjoc.9.171
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/23946849?dopt=Abstract

Alternate JournalBeilstein J Org Chem
PubMed ID23946849
PubMed Central IDPMC3740683
Grant ListR03 MH086456 / MH / NIMH NIH HHS / United States
U54 HG005032 / HG / NHGRI NIH HHS / United States