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The development of a fast and novel methodology to generate carbon-11 carbon monoxide ([ 11 C]CO) from cyclotron-produced carbon-11 carbon dioxide ([ 11 C]CO 2 ) mediated by a fluoride-activated disilane species is described. This methodology allows up to 74 % conversion of [ 11 C]CO 2 to [ 11 C]CO using commercially available reagents, readily available laboratory equipment and mild reaction conditions (room temperature). As proof of utility, radiochemically pure [carbonyl- 11 C]N-benzylbenzamide was successfully synthesized from produced [ 11 C]CO in up to 74 % radiochemical yield (RCY) and >99 % radiochemical purity (RCP) in ≤10 min from end of [ 11 C]CO 2 delivery., (© 2017 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.)

Prion diseases are fatal neurodegenerative and infectious disorders for which effective pharmacological tools are not yet available. This unmet challenge and the recently proposed interplay between prion diseases and Alzheimer's have led to a more urgent demand for new antiprion agents. Herein, we report the identification of a novel bifunctional diketopiperazine (DKP) derivative 1 d, which exhibits activity in the low micromolar range against prion replication in ScGT1 cells, while showing low cytotoxicity. Supported by properly addressed molecular modeling studies, we hypothesized that a planar conformation is the major determinant for activity in this class of compounds. Moreover, studies aimed at assessing the mechanism-of-action at the molecular level showed that 1 d might interact directly with recombinant prion protein (recPrP) to prevent its conversion to the pathogenic misfolded prion protein (PrP(Sc))-like form. This investigation suggests that DKP based antiprion compounds can serve as a promising lead scaffold in developing new drugs to combat prion diseases.