Zhang Hui-Zhen, Zhao Zhi-Long, Zhou Cheng-He
School of Pharmacy, Linyi University, Linyi 276000, China.
School of Pharmacy, Linyi University, Linyi 276000, China.
Eur J Med Chem. 2018 Jan 20;144:444-492. doi: 10.1016/j.ejmech.2017.12.044. Epub 2017 Dec 14.
Oxazole compounds containing nitrogen and oxygen atoms in the five-membered aromatic ring are readily able to bind with a variety of enzymes and receptors in biological systems via diverse non-covalent interactions, and thus display versatile biological activities. The related researches in oxazole-based derivatives including oxazoles, isoxazoles, oxazolines, oxadiazoles, oxazolidones, benzoxazoles and so on, as medicinal drugs have been an extremely active topic, and numerous excellent achievements have been acquired. Noticeably, a large number of oxazole compounds as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have shown their large development value and wide potential as medicinal agents. This work systematically reviewed the recent researches and developments of the whole range of oxazole compounds as medicinal drugs, including antibacterial, antifungal, antiviral, antitubercular, anticancer, anti-inflammatory and analgesic, antidiabetic, antiparasitic, anti-obesitic, anti-neuropathic, antioxidative as well as other biological activities. The perspectives of the foreseeable future in the research and development of oxazole-based compounds as medicinal drugs are also presented. It is hoped that this review will serve as a stimulant for new thoughts in the quest for rational designs of more active and less toxic oxazole medicinal drugs.
五元芳香环中含有氮原子和氧原子的恶唑化合物能够通过多种非共价相互作用与生物系统中的多种酶和受体结合,从而展现出多样的生物活性。基于恶唑的衍生物,包括恶唑、异恶唑、恶唑啉、恶二唑、恶唑烷酮、苯并恶唑等作为药物的相关研究一直是一个极其活跃的课题,并取得了众多优异成果。值得注意的是,大量恶唑化合物作为临床药物或候选药物经常被用于治疗各类疾病,显示出其作为药物的巨大开发价值和广阔潜力。本文系统综述了作为药物的各类恶唑化合物的最新研究进展,包括抗菌、抗真菌、抗病毒、抗结核、抗癌、抗炎和镇痛、抗糖尿病、抗寄生虫、抗肥胖、抗神经病变、抗氧化以及其他生物活性。还介绍了基于恶唑的化合物作为药物研发的可预见未来的前景。希望这篇综述能激发新思路,以合理设计出活性更高、毒性更低的恶唑类药物。