A matrix-focused structure-activity and binding site flexibility study of quinolinol inhibitors of botulinum neurotoxin serotype A

Add time:09/03/2019    Source:sciencedirect.com

Our initial discovery of 8-hydroxyquinoline inhibitors of BoNT/A and separation/testing of enantiomers of one of the more active leads indicated considerable flexibility in the binding site. We designed a limited study to investigate this flexibility and probe structure-activity relationships; utilizing the Betti reaction, a 36 compound matrix of quinolinol BoNT/A LC inhibitors was developed using three 8-hydroxyquinolines, three heteroaromatic amines, and four substituted benzaldehydes. This study has revealed some of the most effective quinolinol-based BoNT/A inhibitors to date, with 7 compounds displaying IC50 values ⩽1 μM and 11 effective at ⩽2 μM in an ex vivo assay.

We also recommend Trading Suppliers and Manufacturers of 8-QUINOLINOL, 7-AMINO-5-CHLORO- (cas 18471-93-7). Pls Click Website Link as below: cas 18471-93-7 suppliers

Prev:Cu(I) coordination polymer based on pyridyl-functionalized resorcin[4]arene: Selective detection of Cr2O72−, MnO4− and nitrobenzene and efficient catalyst for azide–alkyne cycloaddition reaction
Next:Liquid chromatography of phenols on an 8-quinolinol silica gel—iron(III) stationary phase)