α-Amino-α´-Halomethylketones: Synthetic Methodologies and Pharmaceutical Applications as Serine and Cysteine Protease Inhibitors

Title:α-Amino-α´-Halomethylketones: Synthetic Methodologies and Pharmaceutical Applications as Serine and Cysteine Protease Inhibitors

Volume: 13 Issue: 7

Author(s): Vittorio Pace, Laura Castoldi and Massimo Pregnolato

Affiliation:

Keywords: Aminoketones, Drug Synthesis, Haloketones, Inhibitors, Proteases, Structure-activity Relationship.

Abstract: α-Amino-α´-halomethylketones are interesting scaffolds bearing (at least) two sequential electrophilic carbons that by interacting with the nucleophilic moieties of several enzymes, represent the ideal candidates for in vivo and in vitro inhibition studies. In this work a summary of their use as optimal inhibitors of physiologically relevant serine and cysteine proteases is given with a particular emphasis on recently established SAR studies. A brief survey of the most relevant synthetic processes for their obtainment and the importance they possess in synthetic medicinal chemistry is reported.

Cite this article as:

Pace Vittorio, Castoldi Laura and Pregnolato Massimo, α-Amino-α´-Halomethylketones: Synthetic Methodologies and Pharmaceutical Applications as Serine and Cysteine Protease Inhibitors, Mini-Reviews in Medicinal Chemistry 2013; 13 (7) . https://dx.doi.org/10.2174/1389557511313070004