Design and synthesis of xanthine analogues as potent and selective PDE5 inhibitors
作者： Yuguang Wang , Samuel Chackalamannil , Zhiyong Hu , Craig D Boyle , Claire M Lankin
DOI: 10.1016/S0960-894X(02)00646-7
关键词: Stereochemistry 、 Enzyme inhibitor 、 IC50 、 In vivo 、 Bicyclic molecule 、 Chemical synthesis 、 In vitro 、 Enzyme 、 Xanthine 、 Chemistry
摘要: Abstract We have discovered potent and selective xanthine PDE5 inhibitors. Compound 25 (PDE5 IC50=0.6 nM, PDE6/PDE5=101) demonstrated similar functional efficacy PK profile to Sildenafil IC50=3.5 PDE6/PDE5=7).
elsevier.com
sci-hub.se 参考文章(5)
Kathleen A Cox, Kimberly Dunn-Meynell, Walter A Korfmacher, Lisa Broske, Amin A Nomeir, Chin-Chung Lin, Mitchell N Cayen, William H Barr, Novel in vivo procedure for rapid pharmacokinetic screening of discovery compounds in rats Drug Discovery Today. ,vol. 4, pp. 232- 237 ,(1999) , 10.1016/S1359-6446(98)01299-9
Yingzhi Bi, Patrick Stoy, Leonard Adam, Bin He, John Krupinski, Diane Normandin, Ron Pongrac, Laurie Seliger, Andrew Watson, John E Macor, The discovery of novel, potent and selective PDE5 inhibitors. Bioorganic & Medicinal Chemistry Letters. ,vol. 11, pp. 2461- 2464 ,(2001) , 10.1016/S0960-894X(01)00466-8
Heather D. Langtry, Anthony Markham, Sildenafil: a review of its use in erectile dysfunction Drugs. ,vol. 57, pp. 967- 989 ,(1999) , 10.2165/00003495-199957060-00015
Alan Gibson, Phosphodiesterase 5 inhibitors and nitrergic transmission—from zaprinast to sildenafil European Journal of Pharmacology. ,vol. 411, pp. 1- 10 ,(2001) , 10.1016/S0014-2999(00)00824-4
Jackie D. Corbin, Sharron H. Francis, Cyclic GMP phosphodiesterase-5: target of sildenafil. Journal of Biological Chemistry. ,vol. 274, pp. 13729- 13732 ,(1999) , 10.1074/JBC.274.20.13729