4.7 Article

Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY
Volume 21, Issue 8, Pages 2370-2378

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.01.067

Keywords

Phosphodiesterase 7; Quinazoline; Biphenyls

Funding

  1. Almirall Prodesfarma S.A.

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The latest scientific findings concerning PDE7 and PDE4 inhibition suggest that selective small-molecule inhibitors of both enzymes could provide a novel approach to treat a variety of immunological diseases. In this context, we describe a new series of quinazoline derivatives from quinazolin-4-thiones which include a substituted biphenyl fragment. Some of these compounds show inhibitory potencies at sub-micromolar levels against the catalytic domain of PDE7. (C) 2013 Elsevier Ltd. All rights reserved.

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