Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships

Hing L Sham; Chen Zhao; Leping Li; David A Betebenner; Ayda Saldivar; Sudthida Vasavanonda; Dale J Kempf; Jacob J Plattner; Daniel W Norbeck

doi:10.1016/s0960-894x(02)00643-1

Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3101-3. doi: 10.1016/s0960-894x(02)00643-1.

Authors

Hing L Sham¹, Chen Zhao, Leping Li, David A Betebenner, Ayda Saldivar, Sudthida Vasavanonda, Dale J Kempf, Jacob J Plattner, Daniel W Norbeck

Affiliation

¹ Pharmaceutical Discovery, R47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. [email protected]

PMID: 12372511
DOI: 10.1016/s0960-894x(02)00643-1

Abstract

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.

MeSH terms

Cell Line
HIV Protease Inhibitors / chemical synthesis*
HIV Protease Inhibitors / pharmacology*
HIV-1 / drug effects
HIV-1 / enzymology
Humans
Lopinavir
Microbial Sensitivity Tests
Pyrimidinones / chemical synthesis*
Pyrimidinones / pharmacology*
Structure-Activity Relationship

Substances

HIV Protease Inhibitors
Pyrimidinones
Lopinavir