4.5 Article

Bioactive sulfoximines: Syntheses and properties of Vioxx® analogs

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 16, Pages 4888-4890

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.029

Keywords

Sulfoximine; Vioxx (R) (Rofecoxib); hERG activity; COX-2-selective inhibitor (COXIB)

Funding

  1. Fonds der Chemischen Industrie

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The syntheses and biological profiles of sulfoximine-based Vioxx (R) analogs 2 are described. Interesting data have been obtained for 2a, which shows a selective COX-2 inhibition (albeit not as strong as Vioxx (R) itself) exhibiting reduced hERG activity compare to the parent sulfone Vioxx (R) (1). (C) 2011 Elsevier Ltd. All rights reserved.

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