Optimization of N-benzyl-5-nitrofuran-2-carboxamide as an antitubercular agent was written by Gallardo-Macias, Ricardo;Kumar, Pradeep;Jaskowski, Mark;Richmann, Todd;Shrestha, Riju;Russo, Riccardo;Singleton, Eric;Zimmerman, Matthew D.;Ho, Hsin Pin;Dartois, Veronique;Connell, Nancy;Alland, David;Freundlich, Joel S.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2019.Recommanded Product: 37812-51-4 This article mentions the following:
The optimization campaign for a nitrofuran antitubercular hit (N-benzyl-5-nitrofuran-2-carboxamide; JSF-3449) led to the design, synthesis, and biol. profiling of a family of analogs. These compounds exhibited potent in vitro antitubercular activity (MIC = 0.019-0.20 μM) against the Mycobacterium tuberculosis H37Rv strain and low in vitro cytotoxicity (CC50 = 40- > 120 μM) towards Vero cells. Significant improvements in mouse liver microsomal stability and mouse pharmacokinetic profile were realized by introduction of an α,α-dimethylbenzyl moiety. Among these compounds, JSF-4088 (I) is highlighted due to its in vitro antitubercular potency (MIC = 0.019 μM) and Vero cell cytotoxicity (CC50 > 120 μM). The findings suggest a rationale for the continued evolution of this promising series of antitubercular small mols. In the experiment, the researchers used many compounds, for example, 4-(Morpholinomethyl)benzonitrile (cas: 37812-51-4Recommanded Product: 37812-51-4).
4-(Morpholinomethyl)benzonitrile (cas: 37812-51-4) belongs to nitriles. Nitrile compounds can be prepared by the incorporation of a cyanide source through C–C bond formation or by dehydration of primary carboxamides. Industrially, the main methods for producing nitriles are ammoxidation and hydrocyanation. Both routes are green in the sense that they do not generate stoichiometric amounts of salts.Recommanded Product: 37812-51-4
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts