Design, synthesis, and biological testing of potential heme-coordinating nitric oxide synthase inhibitors
…, P Martásek, LJ Roman, RB Silverman
文献索引:Litzinger, Elizabeth A.; Martasek, Pavel; Roman, Linda J.; Silverman, Richard B. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 9 p. 3185 - 3198
Based on computer modeling of the active site of nitric oxide synthases (NOS), a series of 10 amidine compounds (9–18) was designed including potential inhibitors that involve the coordination of side-chain functional groups with the iron of the heme cofactor. The most potent and selective compound was the methylthio amidine analogue 9, which was more potent than l-nitroarginine with 185-fold selectivity for inhibition of neuronal NOS over ...