Potent and selective P2–P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1′, P1, and/or P3 substitutions

One‐pot synthesis of [11C]ureas via triphenylphosphinimines

“…For example, the application of resin-bound triphenylphosphinimines, 27 subjection of amines on solid support 31,32 to the intermediate [ 11 C]isocyanate, as well as the use of a wide range of other nucleophiles that can lead to compounds other than ureas (i.e. thiols, [33][34][35] alkynes, 36,37 or alcohols/acids [38][39][40][41] ). So, the present method generates great possibilities for the preparation of a large number of different 11 C-labeled compounds that can be prepared from […”

Emerging Roles of Cysteine Cathepsins in Disease and their Potential as Drug Targets

“…Researchers at GlaxoSmithKline published a great deal of information about their preclinical research, suggesting that they were the most active in the field. They have been exploring largely all the subsites and different warheads [138,182,[187][188][189][190][191][192][193][194][195][196][197]. The major conclusion was that the most promising compounds are the ketones and the nitriles [138].…”

The effect of molecules in mother-of-pearl on the decrease in bone resorption through the inhibition of osteoclast cathepsin K

“…For example, bisphosphonates cause the apoptosis of osteoclasts which results in failure of the subsequent bone reformation process that is essential to maintain bone quality [16]. To cause the specific inhibition of cathepsin K would be a useful strategy as it does not put osteoclastic functions in jeopardy [15,17].…”