Huanghuai University, College of Chemistry and Pharmaceutical Engineering, Zhumadian, PR China.
Huanghuai University, College of Chemistry and Pharmaceutical Engineering, Zhumadian, PR China.
Eur J Med Chem. 2019 May 15;170:225-234. doi: 10.1016/j.ejmech.2019.03.023. Epub 2019 Mar 15.
Fungi, which can cause serious infections, results in more than 1.35 million deaths annually throughout the world. Azole antifungal drugs which could inhibit the enzyme lanosterol 14α-demethylase, occupy an important position in the treatment of fungal infections. Tetrazoles, practically non-metabolized bioisosteric analog of carboxylic acid and cis-amide, possess a variety of chemotherapeutic properties, including antifungal activities. Hybridization represents a promising strategy to develop novel drugs, and hybridization of tetrazole with other antifungal pharmacophores has the potential to increase the activity and overcome the drug resistance. Various tetrazole hybrids have been designed, synthesized and screened for their antifungal activities, and some of them showed promising activity against both drug-susceptible and drug-resistant fungi. In this review, we present tetrazole hybrids for fighting against fungi. The structure-activity relationship (SAR) is also discussed to provide an insight for rational designs of more effective candidates.
真菌可导致严重感染，每年在全球导致超过 135 万人死亡。唑类抗真菌药物可抑制酶羊毛甾醇 14α-脱甲基酶，在真菌感染的治疗中占有重要地位。四唑类化合物是羧酸和顺酰胺的实际非代谢生物等排体类似物，具有多种化疗特性，包括抗真菌活性。杂化代表了开发新型药物的一种很有前途的策略，将四唑与其他抗真菌药效团杂化有可能提高活性并克服耐药性。已经设计、合成了各种四唑杂化物，并对其抗真菌活性进行了筛选，其中一些对药物敏感和耐药真菌均显示出有希望的活性。在本文中，我们介绍了用于对抗真菌的四唑杂化物。还讨论了结构-活性关系 (SAR)，为设计更有效的候选药物提供了深入了解。
