Author/Authors :
William D. Shrader، نويسنده , , Wendy B. Young، نويسنده , , Paul A. Sprengeler، نويسنده , , Joan C. Sangalang، نويسنده , , Kyle Elrod، نويسنده , , Grant Carr، نويسنده ,
Abstract :
A neutral inhibitor of the serine protease factor Xa was identified via a high-throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Initial modeling efforts and the generation of a series of analogues of 1 are described.