Structural Consequences of the 1,2,3‐Triazole as an Amide Bioisostere in Analogues of the Cystic Fibrosis Drugs VX‐809 and VX‐770,ChemMedChem

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Structural Consequences of the 1,2,3‐Triazole as an Amide Bioisostere in Analogues of the Cystic Fibrosis Drugs VX‐809 and VX‐770
ChemMedChem ( IF 3.6 ) Pub Date : 2020-09-02 , DOI: 10.1002/cmdc.202000650
Jake E. Doiron ₁ , Christina A. Le ₂ , John Bacsa ₃ , Gary W. Breton ₁ , Kenneth L. Martin ₁ , Stephen G. Aller ₂ , Mark Turlington ₁

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The Cover Feature shows a representation of the subtle structural differences between the trans‐amide and 1,2,3‐triazole bioisosteres. As amide looks into the mirror and sees triazole, the question arises: do they look alike? Below the cartoon is an X‐ray structure of an amide‐containing cystic fibrosis drug. The atoms in yellow highlight the drug's planar structure. Above the cartoon is an X‐ray structure of the notably less planar triazole analog. The image background is the region of the cystic fibrosis transmembrane conductance regulator (CFTR) in which these drugs bind. A description of the subtle structural differences between the amide and triazole can be found in the Full Paper by Jake E. Doiron, Christina A. Le, Stephen G. Aller, Mark Turlington et al.

中文翻译：

在囊性纤维化药物VX-809和VX-770的类似物中，1,2,3-三唑作为酰胺类生物等排物的结构后果

封面特征显示了反式酰胺和1,2,3-三唑生物等位基因之间微妙的结构差异。当酰胺看着镜子并看到三唑时，出现了一个问题：它们看起来相似吗？在动画片下方是含酰胺的囊性纤维化药物的X射线结构。黄色的原子突出了药物的平面结构。在动画片上方是平面不太明显的三唑类似物的X射线结构。图像背景是这些药物结合的囊性纤维化跨膜电导调节剂（CFTR）的区域。可以在Jake E. Doiron，Christina A. Le，Stephen G. Aller，Mark Turlington等人的论文全文中找到对酰胺和三唑之间微妙结构差异的描述。

更新日期：2020-09-14

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