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

ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans.
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DOI:
10.3762/bjoc.9.171
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发表时间:
2013
影响因子:
2.7
通讯作者:
Munoz B
Munoz B
中科院分区:
化学4区
文献类型:
--
作者:
Youngsaye 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

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美国国立卫生研究院分子文库和探针生产中心网络(NIH-MLPCN)筛选了30万种化合物,以评估它们在耐药白色念珠菌分离株中恢复氟康唑敏感性的能力。附加的计数筛被用于去除对哺乳动物或真菌细胞固有毒性的物质。一个具有理想生物活性的取代吲哚唑被选中进行进一步的开发,初步的构效关系研究导致ML212的发现。
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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