With the increasing risk of invasive and life threating fungal infections, there is now a great concern regarding the lower discovery rate of antifungal drugs in comparison to antimicrobial agents. Drugs conventionally used in clinics are not adequate enough to combat the increasing fungal infections, especially fungal forms resistant to fluconazole. Among the limited antifungal agents in clinics, azoles have the largest number of drug candidates in clinical trials and are partly marketed due to the particular focus of pharmaceutical companies and medicinal scientific centers. With the rise in the number of papers on azole antifungal design and discovery, a more in-depth understanding the most recent and authentic information about this class of drugs might be beneficial. To this end, we for the first time summarized the state-of-the-art information about azole drugs, with a specific focus on those in the pipelines of pharmaceutical companies, into four generations with regard to their structural similarity. More importantly, this review highlights information on the structure activity relationship (SAR), target description, hybrid antifungal agents as possible future generation, and other useful issues to streamline research towards designing new efficient azole antifungal structures in future.

随着侵入性和威胁生命的真菌感染的风险增加，与抗微生物剂相比，抗真菌药物的发现率越来越低，这引起了人们的极大关注。临床上常规使用的药物不足以抵抗不断增加的真菌感染，尤其是对氟康唑耐药的真菌形式。在临床上有限的抗真菌药物中，唑类药物在临床试验中的候选药物数量最多，由于制药公司和医学科学中心的特别关注，其部分上市。随着关于吡咯类抗真菌药设计和发现的论文数量的增加，更深入地了解有关此类药物的最新信息和真实信息可能会有所帮助。为此，我们首次将关于吡咯类药物的最新信息进行了总结，特别是针对制药公司正在开发的唑类药物，其结构相似性分为四代。更重要的是，本综述重点介绍了有关结构活性关系（SAR），目标描述，可能的下一代抗真菌剂的信息以及其他有用的问题，这些信息有助于简化研究，以期将来设计新型高效的唑类抗真菌结构。