An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology.

Deshpande MS; Wei J; Luo G; Cianci C; Danetz S; Torri A; Tiley L; Krystal M; Yu K; Huang S; Gao Q; Meanwell NA

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An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology.

机译：一种使用平行合成方法鉴定流感病毒融合有效抑制剂的方法。

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Structure-activity studies associated with the salicylic acid-derived inhibitor of influenza fusion, BMY-27709, were examined using a parallel synthesis approach. This SAR survey led to the discovery of potent influenza inhibitory activity in a series of aromatic amides and thioamides derived from 1,3,3-trimethyl-5-hydroxycyclohexylmethylamine. Select compounds were characterized as inhibitors of the H1 subtype of influenza A viruses that act by preventing the pH-induced fusion process, thereby blocking viral entry into host cells. In a plaque-reduction assay, the most potent inhibitors displayed EC(50) values of 0.02-0.14 &mgr;g/mL.

机译：使用平行合成方法检查了与水杨酸衍生的流感融合抑制剂BMY-27709相关的结构活性研究。这项SAR调查导致发现了从1,3,3-三甲基-5-羟基环己基甲胺衍生的一系列芳族酰胺和硫代酰胺具有强大的流感抑制活性。选择的化合物被表征为甲型流感病毒H1亚型的抑制剂，可通过阻止pH诱导的融合过程发挥作用，从而阻止病毒进入宿主细胞。在噬菌斑减少试验中，最有效的抑制剂显示EC（50）值为0.02-0.14 mg / mL。

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来源
《Bioorganic and Medicinal Chemistry Letters》 |2001年第17期|共4页
作者
Deshpande MS; Wei J; Luo G; Cianci C; Danetz S; Torri A; Tiley L; Krystal M; Yu K; Huang S; Gao Q; Meanwell NA;
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正文语种 eng
中图分类药学;生物化学;
关键词
Approaches; inhibitors; Fusion; NOS;

机译：途径;抑制剂;融合;NOS;

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1. An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology. [J] . Deshpande MS, Wei J, Luo G, Bioorganic and Medicinal Chemistry Letters . 2001,第17期

机译：一种使用平行合成方法鉴定流感病毒融合有效抑制剂的方法。
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An approach to the identification of potent inhibitors of influenza virus fusion using parallel synthesis methodology.

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