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

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

Affiliation

  • 1 Pharmaceutical Discovery, D47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. hing.l.sham@abbott.com
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.

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