Azide group biological properties

As part of a systematic search for benzodiazepines exhibiting unusual pharmacological properties, scientists at Hoffman-La Roche synthesized a number of novel azido-substituted benzodiazepine derivatives [291]. The introduction of an azido group in the 7-position of 5-phenyl-1,4-benzodiazepines afforded a series of compounds (225)-(231) which included the 7-azido analogues of diazepam and oxazepam (228) and (229). The azido pharmacophore endowed potency and a spectrum of biological activity comparable with the corresponding 7-halo and 7-nitro analogues, and far superior to the 7-amino derivatives. All of the azides prepared were... 

Click chemistry is commonly used in organic synthesis due to its high yield and its rapid kinetic. Although Cu-catalyzed allqme-azide cycload-dition, also called CuAAC, is the most utilized one, " " the intrinsic toxicity of the copper catalyst and its associated removal difficulties limit its application in biology. For instance, to improve dendrimer s water solubility, PEG groups are often incorporated via this method but a recent study conducted by Week and coworkers has observed substantial copper contamination in them. Copper-free strain promoted allq ne-azide cycloaddition (SPAAC) has been more and more employed to avoid this drawback.Nevertheless this last method introduces rigid cyclooctatriazole units that can modify the dendrimer scaffold and thus its properties. 

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