Inhibition of HIV-1 fusion by hydrogen-bond-surrogate-based α helices

Article abstract of DOI:10.1002/anie.200704227

Inhibition with a twist: An artificial α helix obtained by replacing an N-terminal main-chain i and i+4 hydrogen bond with a carbon-carbon bond (see structure) inhibits gp41-mediated cell fusion. This work suggests that hydrogen-bond-surrogate-derived helices may provide a general class of scaffolds for the generation of leads against viral entry. (Chemical Equation Presented).