Exploring Ugi-Azide Four-Component Reaction Products for Broad-Spectrum Influenza Antivirals with a High Genetic Barrier to Drug Resistance was written by Zhang, Jiantao;Hu, Yanmei;Foley, Christopher;Wang, Yuanxiang;Musharrafieh, Rami;Xu, Shuting;Zhang, Yongtao;Ma, Chunlong;Hulme, Christopher;Wang, Jun. And the article was included in Scientific Reports in 2018.Product Details of 17403-09-7 This article mentions the following:
Influenza viruses are respiratory pathogens that are responsible for seasonal influenza and sporadic influenza pandemic. The therapeutic efficacy of current influenza vaccines and small mol. antiviral drugs is limited due to the emergence of multidrug-resistant influenza viruses. In response to the urgent need for the next generation of influenza antivirals, we utilized a fast-track drug discovery platform by exploring multi-component reaction products for antiviral drug candidates. Specifically, mol. docking was applied to screen a small mol. library derived from the Ugi-azide four-component reaction methodol. for inhibitors that target the influenza polymerase PAC-PB1N interactions. One hit compound 5 was confirmed to inhibit PAC-PB1N interactions in an ELISA assay and had potent antiviral activity in an antiviral plaque assay. Subsequent structure-activity relationship studies led to the discovery of compound 12a, which had broad-spectrum antiviral activity and a higher in vitro genetic barrier to drug resistance than oseltamivir. Overall, the discovery of compound 12a as a broad-spectrum influenza antiviral with a high in vitro genetic barrier to drug resistance is significant, as it offers a second line of defense to combat the next influenza epidemics and pandemics if vaccines and oseltamivir fail to confine the disease outbreak. In the experiment, the researchers used many compounds, for example, 3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7Product Details of 17403-09-7).
3-(Piperidin-4-yl)-1H-indole (cas: 17403-09-7) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Product Details of 17403-09-7
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem