Author/Authors :
Sompong Wattanasin، نويسنده , , Rainer Albert، نويسنده , , Claus Ehrhardt، نويسنده , , Didier Roche، نويسنده , , Michael Sabio، نويسنده , , Ulrich Hommel، نويسنده , , Karl Welzenbach، نويسنده , , Gabriele Weitz-Schmidt، نويسنده ,
Abstract :
The design, synthesis, and biological evaluation of 1,4-diazepane-2-ones as novel LFA-1 antagonists from a scaffold-based combinatorial library are described. Initial optimization of the library lead has resulted in high-affinity antagonists of the LFA-1/ICAM-1 interaction, such as compounds 18d and 18e with IC50 values of 110 and 70 nM, respectively.
