4 research outputs found
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group
A novel HIV protease inhibitor was
designed using a morpholine
core as the aspartate binding group. Analysis of the crystal structure
of the initial lead bound to HIV protease enabled optimization of
enzyme potency and antiviral activity. This afforded a series of potent
orally bioavailable inhibitors of which MK-8718 was identified as
a compound with a favorable overall profile