旨在发现用于治疗勃起功能障碍的选择性磷酸二酯酶5抑制剂的多环鸟嘌呤衍生物的构效关系研究
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
作者信息
Pissarnitski Dmitri A, Asberom Theodros, Boyle Craig D, Chackalamannil Samuel, Chintala Madhu, Clader John W, Greenlee William J, Hu Yueqing, Kurowski Stanley, Myers Joyce, Palamanda Jairam, Stamford Andrew W, Vemulapalli Subbarao, Wang Yuguang, Wang Peng, Wu Ping, Xu Ruo
机构信息
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2004 Mar 8;14(5):1291-4. doi: 10.1016/j.bmcl.2003.12.027.
PMID:14980684
Abstract
Development of structure-activity relationship of cyclic guanines I lead us to discovery of a potent and selective series of phosphodiesterase 5 inhibitors 52-59 (IC50=1.3-11.0 nM, PDE6/5=116-600).
摘要
环鸟嘌呤I的构效关系研究使我们发现了一系列高效且具选择性的磷酸二酯酶5抑制剂52 - 59（IC50 = 1.3 - 11.0 nM，PDE6/5 = 116 - 600）。
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