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Synthesis of Bioactive Heterocyclic Compounds
Published in Ahindra Nag, Greener Synthesis of Organic Compounds, Drugs and Natural Products, 2022
We have synthesized a series of new N-(11H-Indeno[1,2-b]quinoxalin-11-ylidene)-benzohydrazide and evaluated them for their potential to inhibit the activity of α-glucosidase. This enzyme is involved in the digestion of carbohydrates by hydrolyzing the glycosidic bonds in carbohydrates to liberate free glucose and causing postprandial hyperglycemia. This results in type 2 diabetes mellitus that affects approximately over two billion people worldwide [54]. This health-related problem can be overcome by suppressing hyperglycemia that includes reduction of glucose absorption in the gut. The potent α-glucosidase inhibitors are reported to accomplish this task [55, 56]. The quinoxaline compound [1H-Indeno[1,2-b]quinoxalin-11-one] (36) was synthesized by refluxing an equimolar amount of o-phenylenediamine (34) and ninhydrin (35) using ethanol/acetic acid (1:1) as the solvent, as shown in Scheme 8.6.
Application of sulfuric acid modified nano kaolin as a heterogeneous catalyst for the efficient synthesis of quinoxalines and benzothiazines
Published in Inorganic and Nano-Metal Chemistry, 2022
Azam Karimian, Mahdi Norouzi, Zahra Nasri Fargi
Heterocycles containing sulfur and nitrogen, such as quinoxalines, benzoxazines and benzothiazines, are industrially and biologically essential compounds. The quinoxaline derivatives often use in the dyes, herbicides, and fungicides.[1–3] These heterocycles have the potential ability to use in information storage,[4] fluorescent sensors,[5] and security inks.[6] Also, these compounds act as corrosion inhibitors for ferrous and non-ferrous metals and alloys.[7] In the recent years, the research on the quinoxaline structures has been considered due to their wide range of biological and medicinal activities such as anti-microbial, anti-cancer, anti-viral, anti-fungal, anti-bacterial, anti-diabetic, anti-tubercular and anti-schistosomiasis.[7,8] Quinoxalines also exist in a number of antibiotics, such as echinomycin, levomycin and actinomycin.[9,10]
Radical chemistry of alkyl aluminum with quinoxaline ligands
Published in Journal of Coordination Chemistry, 2018
Saba Hajiali Afzali, Ahmed Alzamly, Rohoullah Firouzi, Ilia Korobkov, Sandro Gambarotta
Poly-condensed aromatic molecules based on pyridine, such as polyazine, display an impressive array of attractive features ranging from tendency to stabilize and promote formation of organic radicals [1], to light-harvesting properties [2], formation of robust coordination compounds [3], photosemiconductive properties [4], etc. In this family of compounds, 2,3-bis(2-pyridyl) quinoxaline (DPQ) is especially versatile, having displayed excellent characteristics as chromophore including for biological applications [5]. Quinoxaline derivatives are also frequently encountered as pharmacologically active substances. Last but not least, substituted quinoxalines find applications as dyes [6], electroluminescent materials [7], semiconducting materials [8] and DNA binding agents [9].
Evaluation of anti-bacterial activity of novel 2, 3-diaminoquinoxaline derivatives: design, synthesis, biological screening, and molecular modeling studies
Published in Egyptian Journal of Basic and Applied Sciences, 2022
Suresh Kumar Suthar, Narendra Singh Chundawat, Girdhar Pal Singh, José M. Padrón, Pavan V. Payghan, Yuvraj Kunwar Jhala
Globally, WHO has documented antimicrobial resistance in many first and second-line medications. [1] Lack of advanced medication, healthcare prescribed most expensive with serve toxicity and even less effective to treat chronic bacterial infection. Because of that, prolonged hospital stays and high cost of treatment with poor outcomes increase the tremendous burden on healthcare and may cause leading cause of death in the future. [2] The most advanced second line, antimicrobial medication (vancomycin and methicillin) has developed resistance against Staphylococcus aureus and a similar trend has been shown in the first line, fluconazole against candida fungal strain. [3] Even though there are many medications existing for antimicrobial treatment, no one causes severe adversative effects [4] such as local inflammation (penicillins), allergic reaction, phototoxicity (tetracyclines), effect on the liver, gray baby disorder, and myelosuppression (chloramphenicol) [5]. The bacterial agent can undergo a mutation that causes resistance to corresponding medication or antibiotics, and finally less effectively binds with target sites like alteration in MOA, chemical alterations of the drug, or by other means. [6] Among that, major threatening is bacteria-produced biofilm to reduced penetration effect or neutralized antibiotics effect. [7,8] Quinoxaline motif is a key structural unit; it exists in various biologically active compounds. In recent research, many small molecules of quinoxaline have a tremendous demand in medicinal chemistry, broadly known as potent antiproliferative and antimicrobial agents. The quinoxaline-bearing antibiotics; including, Triostin A and similar kinds of levomycin and echinomycin to introduce into dsDNA and are advantageously effective toward the bacterial diseases caused by gram-positive bacteria. [9,10]