Functionalized quinoxalinones as privileged structures with broad-ranging pharmacological activities

Dual Inhibitors of AChE and BACE-1 for Reducing Aβ in Alzheimer’s Disease: From In Silico to In Vivo

“…Three of the hits, 1–3, contained a quinoxalinone moiety and one hit, 4, had a closely related (fused) quinazolinone moiety. The literature search on quinoxalinone in AChE and BACE-1 inhibitors gave no results, but the quinazolinone fragment was found in some AChE inhibitors [ 92 ] and was mentioned in a patent for BACE-1 inhibitors (US 2013/0150387 A1) [ 93 ], while functionalized quinoxalinones were considered privileged scaffolds [ 94 ]. However, some similar quinoxaline derivatives were found to inhibit Butyrylcholinesterase [ 95 ].…”

Design and synthesis of new bis(1,2,4-triazolo[3,4-b][1,3,4]thiadiazines) and bis((quinoxalin-2-yl)phenoxy)alkanes as anti-breast cancer agents through dual PARP-1 and EGFR targets inhibition

“…etc. [9][10][11] Interestingly, Erdatinib and Brimodine are quinoxalinebased commercial drugs in the market 12,13 (Fig. 1).…”

“…In addition, quinoxaline derivatives were among the most important class of heterocyclic compounds due to their potent therapeutic applications including anticancer, anti-HIV, antiviral, anti-inflammatory, antibacterial, antiallergic, antioxidant, … etc. 9–11 Interestingly, Erdafitinib and Brimodine are quinoxaline-based commercial drugs in the market 12,13 (Fig. 1).…”

Metal‐ And Light‐Free Direct C‐3 Ketoalkylation of Quinoxalin‐2(1H)‐Ones with Cyclopropanols in Aqueous Medium

“…There are excellent reviews detailing various CH-functionalization strategies and the medicinal importance of quinoxalin-2(1H)-ones have appeared recently. [3,15] Indeed, β-carbonyl alkylation of various N-heterocycles is also considered significant because the resultant β-heteroarylated ketone motifs exist in many natural products and bioactive molecules. Furthermore, they serve as functional building blocks for further useful synthetic elaborations.…”

“…[1] In particular, C-3 functionalized quinoxalin-2(1H)-ones proved to be critical constituents of several therapeutic agents, and they possess a wide range of biological activities such as antibacterial, [2a] aldose reductase & antioxidant, [2b] antitumor, , [2c,d] etc. [3] (Figure 1) Given their immense medicinal importance, convenient synthesis to access C-3 functionalized quinoxalin-2(1H)-ones are of great interest. In the last decade, remarkable advances have been achieved in CH-functionalization strategies, especially the late stage functionalization (LSF), as it provides enormous opportunities in achieving atom & step economy, reaction efficiency, selectivity, and allowing a rapid way to generate a diverse set of compounds, etc.that are critical in the area of drug discovery, material research and molecular imaging.…”