Author/Authors :
B. Moon Kim، نويسنده , , Colleen M. Hanifin، نويسنده , , C. Blair Zartman، نويسنده , , Joseph P. Vacca، نويسنده , , Stuart R. Michelson، نويسنده , , Jiunn H. Lin، نويسنده , , I. -H. Chen، نويسنده , , Kari Vastag، نويسنده , , Paul L. Darke، نويسنده , , Joan A. Zugay، نويسنده , , Emilio A. Emini، نويسنده , , William Schleif، نويسنده , , Paul S. Anderson، نويسنده , , Joel R. Huff، نويسنده ,
Abstract :
As a systematic approach to develop HIV-1 protease inhibitors exhibiting desirable pharmacokinetic profiles, hydroxyethylpiperazine series of inhibitors containing various mono- or dialkyl-substituted pyridylmethyl groups have been examined. Very high enzyme inhibitory potency and antiviral activity in a whole cell assay were observed with these inhibitors and, when administered orally to dogs, selected compounds in this series exhibited prolonged half-lives compared to the non-substituted pyridylmethyl compound 1.
