1263191-84-9Relevant academic research and scientific papers
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,Este, Jose A.,Gonzalo, Encarna,Christ, Frauke,Debyser, Zeger,Botta, Maurizio
, p. 343 - 352 (2012/01/11)
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. Easy as A, B, C: Three new series of salicylic acid derivatives were designed and synthesized to investigate their activity toward HIV-1 integrase. Some of these compounds were obtained with microwave-assisted procedures developed and optimized in our research group, which allowed us to rapidly generate several final compounds of high purity.
Arylation of 2-furyl 4-fluorophenyl ketone: An extension of heck chemistry towards novel integrase inhibitors
Franchi, Luigi,Rinaldi, Marta,Vignaroli, Giulia,Innitzer, Anna,Radi, Marco,Botta, Maurizio
experimental part, p. 3927 - 3933 (2010/12/29)
An optimized procedure for the direct and regioselective arylation of 2-acylfurans has been developed. The versatility of this protocol has been evaluated on a series of aryl and heteroaryl halides, thus obtaining a small collection of 2,5-disubstituted f
