New efavirenz derivatives and 1,2,3-triazolyl-phosphonates as inhibitors of reverse transcriptase of HIV-1.

New efavirenz derivatives and 1,2,3-triazolyl-phosphonates as inhibitors of reverse transcriptase of HIV-1. Curr Top Med Chem. 2018 Oct 29;: Authors: Costa CCP, Boechat N, Bastos MM, da Silva FC, Marttorelli A, Souza TML, Baptista MS, Hoelz LVB, Cafffarenad ER Abstract According to the World Health Organization (WHO), the fight against acquired immunodeficiency syndrome (AIDS) is still one of the most significant challenges facing humanity. Worldwide, it is estimated that 36.7 million people are infected by the human immunodeficiency virus (HIV). Despite the variety of available drugs, the search for new enzymatic inhibitors of HIV is still important due to the presence of adverse effects and the development of resistant strains. Therefore, the present study aimed to design, synthesize, and biologically evaluate novel inhibitors of HIV reverse transcriptase (RT). These compounds were obtained in two series, and compounds in both series contain a 1,2,3-triazole ring in their structures. The compounds in the first series are efavirenz (EFV) analogues with the N-1 position substituted by another important fragment as described in the medicinal chemistry literature on anti-HIV drugs. The second series has a phosphonate chain similar to that in the structure of tenofovir (TDF). The results of the biological evaluation showed that all compounds presented high RT inhibition values and lower or comparable inhibitory concentrations (the conce...
Source: Topics in HIV Medicine - Category: Infectious Diseases Authors: Tags: Curr Top Med Chem Source Type: research