A Review on Multipurpose Potential of Bioactive Heterocycle Quinoxaline

Abstract

In last few decades, nitrogen‐containing heterocycles have maintained their status as an important core of FDA‐approved drugs and medicinally active compounds. Quinoxaline is one such class of nitrogen‐containing scaffold that has become a subject of extensive research as it possess a plethora of biological activities. Molecular hybridization is a versatile and rational approach to drug design that involves the combination of two bioactive molecules possessing distinct intrinsic activity into a single scaffold for enhancing their therapeutic potential. In view of this, the advancement and potential of quinoxaline hybrids bearing thiazole, triazole, oxadiazole, pyrrolizines, pyrazole, etc. have attracted the keen attention of researchers to explore their therapeutic ability against different biological targets. The present review includes the research in the recent years (2018–2023) and addresses the graceful advancements in the studies related to quinoxaline‐based small molecules including their synthetic routes, biological activities and structure‐activity relationships. We anticipate that this review article will provide comprehensive knowledge of pharmacological importance of quinoxaline analogues and will fulfill the need of scientific community in designing and developing efficacious novel molecules.

BPO-promoted [4 + 2] cyclization of enaminones and o-phenylenediamines to 2-acyl quinoxalines via a cascade transamination and C–H amination

“…Quinoxaline, also called 1,4-diazanaphthalene, is a crucial core structure of various macrocyclic antibiotics such as echinomycin, levomycin, and actinoleutin that are known to inhibit growth of Gram-positive bacteria, and are active against various transplantable tumors. 1 A literature survey also discloses that quinoxaline derivatives have a wide spectrum of biological activities, such as antiviral, 2 anticancer, 3 and antibacterial activities. 4 In addition to biological and pharmaceutical effects, molecules containing the quinoxaline unit have been widely used in electroluminescent materials 5 and electrical/photochemical materials.…”

Rhodium(II)-Catalyzed Alkynyl Carbene Insertion into N–H Bonds

“…Whereas quinoxalin-2-one scaffold is a privileged core in bioactive molecules, showing therapeutic activity as antagonist, anticancer, antiviral, etc. (Scheme c) . Probably, the envisioned insertion with chelating 1,2-diamines is incredibly challenging, as they would strongly coordinate with the metal and hence could poison the catalysts.…”