2. Academic Validation
  3. Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands

Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands

  • Bioorg Med Chem Lett. 2006 Apr 1;16(7):1869-73. doi: 10.1016/j.bmcl.2006.01.011.
Arun K Ghosh 1,  Gary Schiltz,  Ramu Sridhar Perali,  Sofiya Leshchenko,  Stephanie Kay,  D Eric Walters,  Yasuhiro Koh,  Kenji Maeda,  Hiroaki Mitsuya
Affiliations

Affiliation

  • 1 Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA. [email protected]
PMID: 16480871 DOI: 10.1016/j.bmcl.2006.01.011
Abstract

A series of novel oxyindole-derived HIV-1 Protease Inhibitors were designed and synthesized based upon our X-ray crystal structure of inhibitor 2 (TMC-114) bound to HIV-1 protease. The effects of substituents, spirocyclic rings, and ring sizes have been investigated. A number of inhibitors exhibited low nanomolar inhibitory potencies against HIV Protease.

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