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Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors
Yuguang Wang1, Samuel Chackalamannil, Zhiyong Hu
1Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. yuguang.wang@spcorp.com
Bioorganic & Medicinal Chemistry Letters
|October 10, 2002
Abstract:
We have discovered potent and selective xanthine PDE5 inhibitors. Compound 25 (PDE5 IC(50)=0.6 nM, PDE6/PDE5=101) demonstrated similar functional efficacy and PK profile to Sildenafil (PDE5 IC(50)=3.5 nM, PDE6/PDE5=7).