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.

含有氮和氧原子的五元芳香环恶唑化合物是能够容易地与各种生物系统中的酶和受体的结合通过多样的非共价相互作用，从而展现出多样化的生物活性。恶唑类，异恶唑类，恶唑啉类，恶二唑类，恶唑烷酮类，苯并恶唑类等恶唑类衍生物的相关研究作为药物一直是极为活跃的课题，并取得了许多优异的成绩。值得注意的是，大量的恶唑化合物作为临床药物或候选物经常被用于治疗各种类型的疾病，它们已经显示出其巨大的开发价值和作为药物的广泛潜力。这项工作系统地回顾了恶唑类化合物作为药物的最新研究进展，包括抗菌，抗真菌，抗病毒，抗结核，抗癌，抗炎和止痛，抗糖尿病，抗寄生虫药，抗肥胖，抗神经病，抗氧化以及其他生物活性。还介绍了在基于恶唑的化合物作为药物的研究和开发中可预见的未来。希望这次审查能激发新思想，以寻求对活性更高，毒性更低的恶唑类药物的合理设计。