Original Articles
Urbain C. KassÃÂÂ
Abstract
Agomelatine, a melatonin-like antidepressant drug based on a naphthalene scaffold, has received considerable attention these last twenty years. This drug molecule undergoes important liver first pass effect and suffers therefore of a short plasma half-life. In an effort to circumvent this drawback, we designed an approch based on the use of a tetraline scaffold to replace the original naphthalene template. Using a concise synthetic method involving a threestep approach and starting a commercially available tetralone precursor,we successfully designed a tetraline scaffold, a pivotal template which could be further elaborated into a compound library of agomelatine analogs. Further work is now under progress along this line.