1.
ACS Med Chem Lett
; 7(7): 702-7, 2016 Jul 14.
Artigo
em Inglês
| MEDLINE
| ID: mdl-27437081
RESUMO
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.