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发现一种新型含硼抗真菌剂5-氟-1,3-二氢-1-羟基-2,1-苯并氧杂硼杂环戊烷(AN2690),用于潜在治疗甲癣。

Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.

作者信息

Baker Stephen J, Zhang Yong-Kang, Akama Tsutomu, Lau Agnes, Zhou Huchen, Hernandez Vincent, Mao Weimin, Alley M R K, Sanders Virginia, Plattner Jacob J

机构信息

Anacor Pharmaceuticals Inc., 1060 East Meadow Circle, Palo Alto, California 94303, USA.

出版信息

J Med Chem. 2006 Jul 27;49(15):4447-50. doi: 10.1021/jm0603724.

DOI:10.1021/jm0603724
PMID:16854048
Abstract

A structure-activity relationship investigation for a more efficacious therapy to treat onychomycosis, a fungal infection of the toe and fingernails, led to the discovery of a boron-containing small molecule, 5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), which is currently in clinical trials for onychomycosis topical treatment.

摘要

一项针对治疗甲癣(一种脚趾甲和手指甲真菌感染)的更有效疗法的构效关系研究,导致发现了一种含硼小分子5-氟-1,3-二氢-1-羟基-2,1-苯并硼唑(AN2690),该分子目前正处于甲癣局部治疗的临床试验阶段。

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Discovery of a new boron-containing antifungal agent, 5-fluoro-1,3-dihydro-1-hydroxy-2,1- benzoxaborole (AN2690), for the potential treatment of onychomycosis.发现一种新型含硼抗真菌剂5-氟-1,3-二氢-1-羟基-2,1-苯并氧杂硼杂环戊烷(AN2690),用于潜在治疗甲癣。
J Med Chem. 2006 Jul 27;49(15):4447-50. doi: 10.1021/jm0603724.
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AN-2690, a novel antifungal for the topical treatment of onychomycosis.AN - 2690,一种用于局部治疗甲癣的新型抗真菌药物。
Curr Opin Investig Drugs. 2007 Aug;8(8):662-8.
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An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.一种抗真菌剂通过将tRNA截留在编辑位点来抑制氨酰tRNA合成酶。
Science. 2007 Jun 22;316(5832):1759-61. doi: 10.1126/science.1142189.
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In Vitro penetration of a novel oxaborole antifungal (AN2690) into the human nail plate.新型氧硼杂环戊烷类抗真菌药(AN2690)在体外对人指甲板的渗透作用。
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Tavaborole topical solution, 5% for the treatment of toenail onychomycosis.5% 他氟硼酸盐外用溶液用于治疗趾甲甲癣。
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Crystal structures of the human and fungal cytosolic Leucyl-tRNA synthetase editing domains: A structural basis for the rational design of antifungal benzoxaboroles.人类和真菌胞质亮氨酰 - tRNA合成酶编辑结构域的晶体结构:抗真菌苯并硼唑合理设计的结构基础。
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In vitro efficacy of tavaborole topical solution, 5% after penetration through nail polish on ex vivo human fingernails.5%他氟硼酸钾外用溶液透过指甲油后在离体人指甲上的体外疗效。
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Low Antifungal Activity of Tavaborole against Yeasts and Molds from Onychomycosis.他扎罗汀对甲真菌病中酵母菌和霉菌的抗真菌活性较低。
Antimicrob Agents Chemother. 2018 Nov 26;62(12). doi: 10.1128/AAC.01632-18. Print 2018 Dec.

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