Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
The identification of 2-pyridinylguanidines (e.g., 27 and 28) as selective inhibitors of urokinase-type plasminogen activator (uPA) is described. The X-ray crystal structure of 27 has been determined, and modelling has been used to predict binding in the enzyme active site.
Barber
Christopher G
CG
Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich, Kent CT13 9NJ, UK. christopher_barber@sandwich.pfizer.com
Dickinson
Roger P
RP
Horne
Valerie A
VA
D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006146:Guanidines / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D011725:Pyridines / Q000737:chemistry*; D014568:Urokinase-Type Plasminogen Activator / Q000037:antagonists & inhibitors*; D014961:X-Ray Diffraction
D004791:Enzyme Inhibitors; D006146:Guanidines; D011725:Pyridines; D014568:Urokinase-Type Plasminogen Activator; C023666:pyridine