Title of article :
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors
Author/Authors :
George D. Hartman، نويسنده , , Mark E. Duggan، نويسنده , , William F. Hoffman، نويسنده , , Robert J. Meissner، نويسنده , , James J. Perkins، نويسنده , , Amy E. Zartman، نويسنده , , Adel M. Naylor-Olsen، نويسنده , , Jacquelynn J. Cook، نويسنده , , Joan D. Glass، نويسنده , , Robert J. Lynch، نويسنده , , Guixiang Zhang، نويسنده , , Robert J. Gould، نويسنده ,
Abstract :
A new series of potent, linearly-minimized, orally active, selective GPIIb/IIIa inhibitors is identified. Thus 15 (L-750,034) achieves interaction via a constrained, non-turned conformation that maintains the proper distance between its charged termini and full sulfonamide exosite interaction. The diminutive stature and the proposed linear conformation of L-750,034 define a new paradigm for the conceptualization of RGD mimics.
