Tetrazole hybrids and their antifungal activities

• Published in: European journal of medicinal chemistry Vol. 170; pp. 225 - 234
• Main Authors: Wang, Sheng-Qiang, Wang, Yan-Fang, Xu, Zhi
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 15.05.2019
• Subjects: Antifungal activity; Fungi; Hybrid compounds; Structure-activity relationship; Tetrazole; Fungi; Antifungal activity; Hybrid compounds; Tetrazole; Structure-activity relationship
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2019.03.023

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. 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. [Display omitted] •This review covers the recent advances of tetrazole hybrids as potential antifungal agents.•Some of them such as VT-1161 and VT-1129 are under clinical trials for the treatment of fungal infections.•The structure-activity relationship was enriched.