1089315-92-3Relevant articles and documents
A concise approach to n-substituted rhodanines through a base-assisted one-pot coupling and cyclization process
Huo, Zhipeng,Liang, Yongxi,Sun, Xun,Tang, Mei-Lin,Zhang, Chenchen
, (2020/03/17)
An efficient approach to obtain functionalized rhodanines was developed through a base-assisted one-pot coupling and continuous cyclization of a primary amine, carbon disulfide, and methyl (2-chloroacetyl)carbamate. This conversion tolerates a broad range of functional groups and can be used to scale the preparation of N-substituted rhodanines in excellent yields.
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
experimental part, 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.
