Synthesis and structure-activity relationships of a novel series of HIV-1 protease inhibitors encompassing ABT-378 (Lopinavir)

  • Bioorg Med Chem Lett. 2002 Apr 22;12(8):1185-7. doi: 10.1016/s0960-894x(02)00134-8.
Hing L Sham  1 ,  David A Betebenner ,  Xiaoqi Chen ,  Ayda Saldivar ,  Sudthida Vasavanonda ,  Dale J Kempf ,  Jacob J Plattner ,  Daniel W Norbeck
Affiliations
  • 1. Pharmaceutical Discovery, D47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. [email protected]
PMID: 11934584 DOI: 10.1016/s0960-894x(02)00134-8
Abstract

The HIV Protease Inhibitor ABT-378 (Lopinavir) has a 2,6-dimethylphenoxyacetyl group in the P-2' position. Analogues in which this group is replaced with various substituted phenyl or heteroaryl groups were synthesized and the structure-activity relationships explored.