Sharma Aastha, Deep Aakash, Marwaha Minakshi Gupta, Marwaha Rakesh Kumar
Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak-124001, Haryana, India.
Department of Pharmaceutical Sciences, Chaudhary Bansi Lal University, Bhiwani 127021, Haryana, India.
Mini Rev Med Chem. 2022;22(6):927-948. doi: 10.2174/1389557521666210927123831.
Quinoxaline (C8H6N2), commonly called 1,4-diazanaphthalene, 1,4-benzodiazine, or benzopyrazine, is a very potent nitrogenous heterocyclic moiety consisting of a benzene ring fused with the pyrazine ring. A number of different methods for the synthesis of quinoxaline derivatives have been reported in the literature, but the most effective method, commonly used for the synthesis of quinoxaline analogues involves the condensation of substituted o-phenylenediamines with 1, 2- dicarbonyl compounds in the presence of different catalyst(s). The presence of different types of catalysts and their concentration affects the overall yield of the product. Quinoxaline not only plays an important role as an organic reaction intermediate but also has a wide spectrum of interesting biological activities viz. antibacterial, antifungal, anticancer, anti-inflammatory, antiviral, and antiprotozoal activity, etc. Some commercially available drug molecules containing quinoxaline moiety are echinomycin (as antibacterial, antineoplastic, and nucleic acid inhibitor), triostins (cyclic desipeptide as an antibacterial agent), dioxidine and mequindox (as antibacterial agents), carbadox (controlling swine dysentery), desoxycarbadox (as swine growth promoter) and panadipion (as hepatoprotective agent), etc. A large number of quinoxaline analogues possessing different biological activities and their synthetic procedures have been patented worldwide.
喹喔啉（C8H6N2），通常称为1,4 - 二氮杂萘、1,4 - 苯并二嗪或苯并吡嗪，是一种非常有效的含氮杂环部分，由一个与吡嗪环稠合的苯环组成。文献中报道了许多合成喹喔啉衍生物的不同方法，但合成喹喔啉类似物最常用的有效方法是在不同催化剂存在下，使取代的邻苯二胺与1,2 - 二羰基化合物缩合。不同类型催化剂的存在及其浓度会影响产物的总产率。喹喔啉不仅作为有机反应中间体发挥重要作用，而且还具有广泛有趣的生物活性，即抗菌、抗真菌、抗癌、抗炎、抗病毒和抗原虫活性等。一些含有喹喔啉部分的市售药物分子有棘霉素（作为抗菌、抗肿瘤和核酸抑制剂）、曲古抑菌素（作为抗菌剂的环缩肽）、二氧喹啉和乙酰甲喹（作为抗菌剂）、卡巴氧（用于控制猪痢疾）、脱氧卡巴氧（作为猪生长促进剂）和泛癸利酮（作为肝脏保护剂）等。大量具有不同生物活性的喹喔啉类似物及其合成方法已在全球获得专利。
