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Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy
Arun K Ghosh1, Lisa M Swanson, Chunfeng Liu
1Department of Chemistry, University of Illinois at Chicago, 60607, USA. arunghos@uic.edu
Bioorganic & Medicinal Chemistry Letters
|July 13, 2002
Abstract:
A series of novel macrocyclic urethanes incorporating a (R)-hydroxyethylamine isostere was designed and synthesized. Ring size and substituent efffects have been investigated. Cyclourethanes containing 14- to 16-membered rings exhibited low nanomolar inhibitory potencies against HIV-1 protease.