ChemMedChem

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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    Dr. Yves P. Auberson, Dr. Cara Brocklehurst, Dr. Markus Furegati, Dr. Thomas C. Fessard, Dr. Guido Koch, Dr. Andrea Decker, Dr. Luigi La Vecchia and Dr. Emmanuelle Briard

    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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