Efficient synthesis of nevirapine analogs to study its metabolic profile by click fishing

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6127-30. doi: 10.1016/j.bmcl.2009.09.011. Epub 2009 Sep 9.

Abstract

Knowledge of the biotransformation and pharmacokinetics of the antiretroviral agent nevirapine is still insufficient. In order to trace rash inducing metabolites of nevirapine, we devised a short and efficient multi-gram synthesis of a nevirapine analog that can be coupled to azide containing compounds by click chemistry.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / metabolism
  • Crystallography, X-Ray
  • Cyclization
  • Humans
  • Molecular Conformation
  • Nevirapine / chemical synthesis*
  • Nevirapine / chemistry
  • Nevirapine / metabolism
  • Rats

Substances

  • Anti-HIV Agents
  • Nevirapine