Iterative oxime bond chemistry leads to protease inhibitors.
[structure: see text] In the present paper, we have looked at iterative coupling as a strategy to form new druglike molecules. We have developed an iterative coupling chemistry based on oxime bond formation between hydroxyaromatic aldehyde building blocks to form linear oxime oligomers. The strategy is validated by the discovery of micromolar protease inhibitors.
Renaudet
Olivier
O
Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, 3012 Bern, Switzerland.
Reymond
Jean-Louis
JL
D002918:Chymotrypsin / Q000378:metabolism; D018360:Crystallography, X-Ray; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D015394:Molecular Structure; D010091:Oximes / Q000737:chemistry*; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology
D010091:Oximes; D011480:Protease Inhibitors; D002918:Chymotrypsin