作为强效和选择性磷酸二酯酶5（PDE5）抑制剂的黄嘌呤类似物的设计与合成。
Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors.
作者信息
Wang Yuguang, Chackalamannil Samuel, Hu Zhiyong, Boyle Craig D, Lankin Claire M, Xia Yan, Xu Ruo, Asberom Theodros, Pissarnitski Dmitri, Stamford Andrew W, Greenlee William J, Skell Jeffrey, Kurowski Stanley, Vemulapalli Subbarao, Palamanda Jairam, Chintala Madhu, Wu Ping, Myers Joyce, Wang Peng
机构信息
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.
出版信息
Bioorg Med Chem Lett. 2002 Nov 4;12(21):3149-52. doi: 10.1016/s0960-894x(02)00646-7.
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).
我们发现了强效且具有选择性的黄嘌呤磷酸二酯酶5（PDE5）抑制剂。化合物25（PDE5半数抑制浓度[IC(50)] = 0.6纳摩尔，PDE6/PDE5 = 101）显示出与西地那非（PDE5 IC(50)=3.5纳摩尔，PDE6/PDE5 = 7）相似的功能疗效和药代动力学特征。
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