Novel lopinavir analogues incorporating heterocyclic replacements of six-member cyclic urea--synthesis and structure-activity relationships

  • Bioorg Med Chem Lett. 2004 May 17;14(10):2643-5. doi: 10.1016/j.bmcl.2004.02.089.
Hing L Sham  1 ,  David A Betebenner ,  William Rosenbrook ,  Thomas Herrin ,  Ayda Saldivar ,  Sudthida Vasavanonda ,  Jacob J Plattner ,  Daniel W Norbeck
Affiliations
  • 1. Pharmaceutical Discovery, R4MA Building AP-10, Abbott Laboratories, Abbott Park, IL 60064-6101, USA. [email protected]
PMID: 15109669 DOI: 10.1016/j.bmcl.2004.02.089
Abstract

The HIV Protease inhibitor ABT-378 (lopinavir) has a six-member cyclic urea in the P-2 position. A series of analogues in which the six-member cyclic urea is replaced by various heterocycles was synthesized and the structure-activity relationships explored.