Bi Y, Stoy P, Adam L, He B, Krupinski J, Normandin D, Pongrac R, Seliger L, Watson A, Macor J E
Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA.
Bioorg Med Chem Lett. 2001 Sep 17;11(18):2461-4. doi: 10.1016/s0960-894x(01)00466-8.
The design and synthesis of a novel scaffold for potent and selective PDE5 inhibitors are described. Compound 3a was more potent (PDE5 IC50=0.31 nM) and selective (>10,000-fold vs PDE1 and 160-fold selective vs PDE6) PDE5 inhibitor than sildenafil.
描述了一种新型强效和选择性PDE5抑制剂支架的设计与合成。化合物3a是一种比西地那非更有效的PDE5抑制剂（PDE5 IC50 = 0.31 nM），且具有选择性（对PDE1的选择性大于10000倍，对PDE6的选择性为160倍）。
