The efavirenz: Structure-activity relantionship and synthesis methods

Abstract

Acquired Immunodeficiency Syndrome (AIDS) is a disease caused by HIV and it affects all continents. Since 1987 an antiretroviral therapy has been used and it increases survival rates and improves patient's quality of life. Efavirenz (EFV) is a widely used drug to treat HIV-AIDS. It belongs to the class of non-nucleoside inhibitors of reverse transcriptase (NNRTI) and blocks the action of the enzyme and the virus multiplication. Although it presents excellent results in reducing viral load, in recent years, resistance cases associated with adverse effects encouraged many research groups to investigate the structure-activity relationship of this drug's novel analogues. Therefore, the current study aims to compare the EFV activity with those of its analogs using medicinal chemistry concepts as well as to show the main synthetic routes in their production.