Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors

Bioorg Med Chem Lett. 1998 Apr 21;8(8):979-82. doi: 10.1016/s0960-894x(98)00139-5.

Abstract

A series of novel spirocyclic ethers were designed to function as nonpeptidal P2-ligands for HIV-1 protease inhibitors. Incorporation of designed ligands in the (R)-(hydroxyethylamino)sulfonamide isostere afforded potent HIV protease inhibitors.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Crystallography, X-Ray
  • Drug Design
  • Ethers, Cyclic / chemical synthesis*
  • Ethers, Cyclic / chemistry*
  • Ethers, Cyclic / pharmacology
  • HIV Protease / metabolism*
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / chemistry*
  • HIV Protease Inhibitors / pharmacology
  • HIV-1 / enzymology
  • Humans
  • Kinetics
  • Ligands
  • Models, Molecular
  • Molecular Conformation
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Ethers, Cyclic
  • HIV Protease Inhibitors
  • Ligands
  • HIV Protease