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2004
Fused pyrimidine derivatives
R 0515
Spiroquinazolinones as Novel, Potent, and Selective PDE7 Inhibitors.
2. Optimization of 5,8-Disubstituted Derivatives. — Preliminary results on the
52- 138 Part
optimization of the substituent at the 5-position of the hydrophobic lead structure
5,8-dichloro-spirocyclohexane-quinazolinone towards PDE7 inhibitors with acceptable pharmacokinetic properties are presented. The neutral (IV), basic (VI), and acidic
(VIII) compounds are potent, selective, and soluble PDE7 inhibitors, and useful to
reveal the functional role of the enzyme PDE7 in vitro. The in vivo pharmacokinetic
profile of the neutral derivative (IV) and acid (VIII) is more favorable than that of the
basic derivative (VI) (no yields given). — (BERNARDELLI*, P.; et al.; Bioorg. Med.
Chem. Lett. 14 (2004) 18, 4627-4631; Aventis Pharm., F-94400 Vitry-sur-Seine, Fr.;
Eng.) — H. Hoennerscheid
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