Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir)

  • Bioorg Med Chem Lett. 2001 Jun 4;11(11):1351-3. doi: 10.1016/s0960-894x(01)00243-8.
H L Sham  1 ,  D A Betebenner ,  T Herrin ,  G Kumar ,  A Saldivar ,  S Vasavanonda ,  A Molla ,  D J Kempf ,  J J Plattner ,  D W Norbeck
Affiliations
  • 1. Pharmaceutical Discovery, D47B, Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. [email protected]
PMID: 11378352 DOI: 10.1016/s0960-894x(01)00243-8
Abstract

The HIV Protease Inhibitor ABT-378 (Lopinavir) is metabolized rapidly and extensively by CYP-3A4 catalyzed oxidation. Three of the major metabolites identified were synthesized and their Antiviral (HIV) activities determined.

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