Skip Navigation
Explore our COVID-19 Resources and Updates
CHS blue logo square
Home > Our Work > All Publications > 2018


Our publications keep professionals informed on the most important developments and issues in health security and biosecurity.

Find an article or report by keywords:

Find an article or report or see all by area, author, or year:


Optimization of N-benzyl-5-nitrofuran-2-carboxamide as an antitubercular agent

Ricardo Gallardo-Macias, Pradeep Kumar, Mark Jaskowski, Todd Richmann, Riju Shrestha, Riccardo Russo, Eric Singleton, Matthew D Zimmerman, Hsin Pin Ho, Véronique Dartois, Nancy Connell, David Alland, Joel S Freundlich
Date posted:
December 24, 2018
Publication type:
Bioorg Med Chem Lett. 2019;29(4):601-606
The optimization campaign for a nitrofuran antitubercular hit (N-benzyl-5-nitrofuran-2-carboxamide; JSF-3449) led to the design, synthesis, and biological 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 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 molecules.



Our Mission

To protect people’s health from epidemics and disasters and ensure that communities are resilient to major challenges.