| Literature DB >> 15837326 |
Craig D Boyle1, Ruo Xu, Theodros Asberom, Samuel Chackalamannil, John W Clader, William J Greenlee, Henry Guzik, Yuequing Hu, Zhiyong Hu, Claire M Lankin, Dmitri A Pissarnitski, Andrew W Stamford, Yuguang Wang, Jeffrey Skell, Stanley Kurowski, Subbarao Vemulapalli, Jairam Palamanda, Madhu Chintala, Ping Wu, Joyce Myers, Peng Wang.
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 41 demonstrated 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.Entities:
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Year: 2005 PMID： 15837326 DOI： 10.1016/j.bmcl.2005.02.083
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823