制备了28种小的阳离子1,4-取代的1,2,3-三唑阳离子文库,用于研究抗菌活性。该结构解决了小型抗菌肽的药效团模型和在海洋抗菌剂中发现的两亲基序的问题。八种化合物显示出令人鼓舞的抗菌活性,其中最有效的化合物10b对无乳链球菌,金黄色葡萄球菌,铜绿假单胞菌,大肠杆菌和粪肠球菌的最低抑制浓度为4–8μg/ mL 。简单的合成和低的官能度使这些1,4-取代的1,2,3-三唑对于进一步的优化很有趣。
制备了28种小的阳离子1,4-取代的1,2,3-三唑阳离子文库,用于研究抗菌活性。该结构解决了小型抗菌肽的药效团模型和在海洋抗菌剂中发现的两亲基序的问题。八种化合物显示出令人鼓舞的抗菌活性,其中最有效的化合物10b对无乳链球菌,金黄色葡萄球菌,铜绿假单胞菌,大肠杆菌和粪肠球菌的最低抑制浓度为4–8μg/ mL 。简单的合成和低的官能度使这些1,4-取代的1,2,3-三唑对于进一步的优化很有趣。
The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
Facile Synthesis of Triazoles using Electrospray‐Deposited Copper Nanomaterials to Catalyze Azide‐Alkyne Cycloaddition (AAC) Click Reactions
作者:Jyotirmoy Ghosh、R. Graham Cooks
DOI:10.1002/cplu.202200252
日期:2022.10
directly onto the liquid surface of the reaction solution, drives the synthesis of triazoles by the azide-alkyne cycloaddition (AAC) click reaction an order of magnitude faster than does the conventional catalyst.Facile Synthesis of Triazoles using Electrospray-Deposited Copper Nanomaterials to Catalyze Azide-Alkyne Cycloaddition (AAC) Click Reactions (J. Ghosh and R. G. Cooks) @AstonlabsPurdue