Cover image for Vol. 12 Issue 6

Editorial Board Chairs: Antonello Mai, Rainer Metternich. Assoc. Editors: David Peralta, Scott Williams (Sr)

Impact Factor: 2.98

ISI Journal Citation Reports © Ranking: 2015: 18/59 (Chemistry Medicinal); 77/255 (Pharmacology & Pharmacy)

Online ISSN: 1860-7187

Associated Title(s): Angewandte Chemie International Edition, Chemistry - A European Journal, Chemistry – An Asian Journal, ChemBioChem, Medicinal Research Reviews, Molecular Informatics

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March 22, 2017

VIP: The Emerging Picture of Sulfoximines in Drug Discovery

VIP: The Emerging Picture of Sulfoximines in Drug DiscoveryJuan Alberto Sirvent, Dr. Ulrich Lücking*

After being neglected for a long time, sulfoximines, the mono-aza analogues of sulfones, have recently gained considerable recognition as a new and versatile structural motif in the life sciences. The synthetic methodology for sulfoximines has progressed significantly over the last decade; however, the general understanding of this functional group regarding its medicinal-chemistry-relevant properties is still limited. Read more...

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    Version of Record online: 27 MAR 2017 | DOI: 10.1002/cmdc.201700082

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    Lifting the fog: Many drug and tracer candidates contain para-substituted phenyl groups, and we show that their physicochemical properties can be improved by bioisosteric substitutions. While bicyclo[2.2.2]octyl has properties similar to those of para-phenyl, the use of bicyclo[1.1.1.]pentyl and cubane-1,4-diyl leads to strongly increased water solubility, and to a marked decrease in nonspecific binding (NSB). This is particularly important for PET imaging tracers, as the lower the NSB signal, the less “foggy” images will be.

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