A versatile and practical synthesis toward the development of novel HIV-1 integrase inhibitors
Rinaldi, Marta Tintori, Cristina Franchi, Luigi Vignaroli, Giulia Innitzer, Anna Massa, Silvio Esté, José A Gonzalo, Encarna Christ, Frauke Debyser, Zeger Botta, Maurizio # ×
Wiley - V C H Verlag GmbH & Co. KGaA
ChemMedChem vol:6 issue:2 pages:343-352
As a continuation of our previous work, which resulted in the identification of a new hit compound as an HIV-1 integrase inhibitor, three novel series of salicylic acid derivatives were synthesized using three versatile and practical synthetic strategies and were assayed for their capacity to inhibit the catalytic activity of HIV-1 integrase. Biological evaluations revealed that some of the synthesized compounds possess good inhibitory potency in enzymatic assays and are able to inhibit viral replication in MT-4 cells at low micromolar concentrations. Finally, docking studies were conducted to analyze the binding mode of the synthesized compounds within the DNA binding site of integrase in order to refine their structure-activity relationships.