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Tetrazole hybrids and their antifungal activities.

Abstract：

: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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wang SQ,Wang YF,Xu Z

doi

10.1016/j.ejmech.2019.03.023

subject

Has Abstract

pub_date

2019-05-15 00:00:00

pages

225-234

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(19)30240-5

journal_volume

170

pub_type

杂志文章,评审

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