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.
Hing L Sham  1 ,  Chen Zhao ,  Leping Li ,  David A Betebenner ,  Ayda Saldivar ,  Sudthida Vasavanonda ,  Dale J Kempf ,  Jacob J Plattner ,  Daniel W Norbeck
Affiliations
  • 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.