Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
The HIV protease inhibitor Lopinavir has a pseudosymmetric core unit incorporating benzyl groups at both P-1, P-1' positions. A series of analogues incorporating non-aromatic side chains at the P-1 position were synthesized and the structure-activity relationships explored.
Sham
Hing L
HL
Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. hing.l.sham@abbott.com
Zhao
Chen
C
Li
Leping
L
Betebenner
David A
DA
Saldivar
Ayda
A
Vasavanonda
Sudthida
S
Kempf
Dale J
DJ
Plattner
Jacob J
JJ
Norbeck
Daniel W
DW
D002460:Cell Line; D017320:HIV Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D061466:Lopinavir; D008826:Microbial Sensitivity Tests; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D017320:HIV Protease Inhibitors; D011744:Pyrimidinones; D061466:Lopinavir