The Retro-2 molecule protects cells against Shiga toxins by specifically blocking retrograde transport from early endosomes to the trans-Golgi network A SAR study has been carried out to identify more potent compounds. Cyclization and modifications of Retro-2 led to a compound with roughly 100 fold improvement of the EC50 against Shiga toxin cytotoxicity measured in a cell protein synthesis assay. We also demonstrated that only one enantiomer of the dihydroquinazolinone reported herein is bioactive.
Furan-2-carbaldehydes as C1 building blocks for the synthesis of quinazolin-4(3<i>H</i>)-ones <i>via</i> ligand-free photocatalytic C–C bond cleavage
作者:Wenjia Yu、Xianwei Zhang、Bingjie Qin、Qiyang Wang、Xuhong Ren、Xinhua He
DOI:10.1039/c8gc00079d
日期:——
efficient green C1 building blocks to synthesize bioactive quinazolin-4(3H)-ones by ligand-free photocatalytic C–C bondcleavage. Notably, protection of hydroxyl, carboxyl, amide, or secondary amino groups is not required. Mechanisticstudies suggest that conjugated N,O-tridentate copper complexes act as novel photoinitiators under visible light.