Author/Authors :
Craig D. Boyle، نويسنده , , Ruo Xu، نويسنده , , Theodros Asberom، نويسنده , , Samuel Chackalamannil، نويسنده , , John W. Clader، نويسنده , , William J. Greenlee، نويسنده , , Henry Guzik، نويسنده , , Yuequing Hu، نويسنده , , Zhiyong Hu، نويسنده , , Claire M. Lankin، نويسنده , , Dmitri A. Pissarnitski، نويسنده , , Andrew W. Stamford، نويسنده , , Yuguang Wang، نويسنده , , Jeffrey Skell، نويسنده , , Stanley Kurowski، نويسنده , , Subbarao Vemulapalli، نويسنده , , Jairam Palamanda، نويسنده , , Madhu Chintala، نويسنده , , Ping Wu، نويسنده , , Joyce Myers، نويسنده , , et al.، نويسنده ,
Abstract :
In search of a PDE5 inhibitor for erectile dysfunction, an SAR was developed from a PDE1/PDE5 purine series of leads, which had modest PDE5 potency and poor isozyme selectivity. A compound (41) with PDE5 inhibition and in vivo activity similar to sildenafil was discovered from this effort. In addition, purine 41demonstrated superior overall PDE isozyme selectivity when compared to the approved PDE5 inhibitors sildenafil, vardenafil, and tadalafil, which may result in a more favorable side-effect profile.
Keywords :
PDE5 inhibitor , Erectile dysfunction , Male ED , Purine