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2004
Fused pyrimidine derivatives
R 0515
Discovery of Thiadiazoles as a Novel Structural Class of Potent and Selective
Inhibitors. Part 1. Design, Synthesis and Structure—Activity Relationship
52- 136 PDE7
Studies. — To optimize the enzymatic inhibitory activity and the selectivity profile, a
thiadiazole based screening hit is modified by replacement of the chlorophenyl group
with aminoquinazoline derivatives. An essential improvement in activity and selectivity is achieved with small molecule PDE7 inhibitors (IX), which display activity in the
low nanomolar range and exhibit high selectivity over PDE4. — (VERGNE*, F.; et
al.; Bioorg. Med. Chem. Lett. 14 (2004) 18, 4607-4613; Aventis Pharm.,
F-94400 Vitry-sur-Seine, Fr.; Eng.) — H. Hoennerscheid
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