doi: 10.1016/j.bmcl.2006.01.011.
Epub 2006 Feb 15.
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands
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- PMID: 16480871
- DOI: 10.1016/j.bmcl.2006.01.011
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Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands
Bioorg Med Chem Lett.
.
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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