Functionalized aliphatic P2/P2' analogs of HIV-1 protease inhibitor DMP323

Abstract A series of analogs of HIV protease inhibitor DMP323 containing functionalized aliphatic P2/P2′ groups was prepared and evaluated for HIV protease inhibition and antiviral activity in a cell-based assay. Asymmetric compounds with a 5-hydroxypentyl substituent at P2 and a benzylic substituent at P2′ showed increased potency over the corresponding symmetrically substituted analogs.