Author/Authors :
B. Moon Kim، نويسنده , , Ben E. Evans، نويسنده , , Kevin F. Gilbert، نويسنده , , Colleen M. Hanifin، نويسنده , , Joseph P. Vacca، نويسنده , , Stuart R. Michelson، نويسنده , , Paul L. Darke، نويسنده , , Joan A. Zugay، نويسنده , , Emilio A. Emini، نويسنده , , William Schleif، نويسنده , , Jiunn H. Lin، نويسنده , , I. -H. Chen، نويسنده , , Kari Vastag، نويسنده , , Paul S. Anderson، نويسنده , , Joel R. Huff، نويسنده ,
Abstract :
A series of HIV-1 protease inhibitors containing various acyclic or cyclic alkylpiperazine derivatives were prepared. They exhibit excellent potency in the enzyme inhibition assay and in a whole cell assay demonstrating the lowest CIC95/IC50 ratios observed in the hydroxyethylpiperazine class of inhibitors. Oral pharmacokinetic studies in dogs have been carried out on two compounds in this series and an excellent oral absorption profile was obtained for inhibitor 13, which possesses a cyclopropylpiperazine unit.
