Bouz, Ghada; Bouz, Sarah; Jandourek, Ondrej; Konecna, Klara; Barta, Pavel; Vinsova, Jarmila; Dolezal, Martin; Zitko, Jan published the artcile< Synthesis, biological evaluation, and in silico modeling of N-substituted quinoxaline-2-carboxamides>, Application In Synthesis of 3959-07-7, the main research area is N substituted quinoxaline 2 carboxamides synthesis; Mycobacterium tuberculosis; antimycobacterial; cytotoxicity; molecular docking; pyrazinamide; quinoxaline; tuberculosis.
Despite the established treatment regimens, tuberculosis remains an alarming threat to public health according to WHO. Novel agents are needed to overcome the increasing rate of resistance and perhaps achieve eradication. As part of our long-term research on pyrazine derived compounds, we prepared a series of their ortho fused derivatives, N-phenyl- and N-benzyl quinoxaline-2-carboxamides, and evaluated their in vitro antimycobacterial activity. In vitro activity against Mycobacterium tuberculosis H37Ra (represented by min. inhibitory concentration, MIC) ranged between 3.91-500μg/mL, with most compounds having moderate to good activities (MIC < 15.625μg/mL). The majority of the active compounds belonged to the N-benzyl group. In addition to antimycobacterial activity assessment, final compounds were screened for their in vitro cytotoxicity. N-(naphthalen-1-ylmethyl)quinoxaline-2-carboxamide (compound 29) was identified as a potential antineoplastic agent with selective cytotoxicity against hepatic (HepG2), ovarian (SK-OV-3), and prostate (PC-3) cancer cells lines. Mol. docking showed that human DNA topoisomerase and vascular endothelial growth factor receptor could be potential targets for 29. Pharmaceuticals published new progress about Antimycobacterial agents. 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Application In Synthesis of 3959-07-7.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary