Xianqing Deng, Haopeng Sun, B. G. Youssif
Feb 1, 2023
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Frontiers in Chemistry
Abstract
Triazole refers to a heterocyclic with molecular formula C2H3N3, having a five-membered ring of two carbon and three nitrogen atoms. It had reported that compounds containing triazole exhibited broad biological activities, such as antimicrobial, analgesic, antiinflammatory, anticonvulsant, antineoplastic, antimalarial, antiviral, antiproliferative, and anticancer activities. The electron richness and aromaticity of triazole enable it to freely bind with a wide range of biomacromolecules by interactions of pi–pi bonds, H bonds, and iondipole bonds. In recent years, the number of research articles on triazole use in medicinal chemistry has increased substantially. Triazoles are becoming potential drug candidates for the scientific community. Regarding the Research Topic, the synthesis method and pharmacological effects of triazole derivatives are very attractive and prospective. Dai et al. summarized the synthetic methods of 1,2,3-/1,2,4-triazoles combined with the progress of triazole over the past 2 decades. Several main synthetic methods from various nitrogen sources were summarized. The synthetic methods were sorted according to the key starting material utilized for the production of the 1,2,3-/1,2,4-triazole backbones, and some new synthetic methods to access triazole derivatives with biological activities were presented. Song et al. discovered a skeleton of triazolopyrimidine for the development of new antiepileptics (AEDs). The design, synthesis, and in vivo anticonvulsant activity evaluation of triazolopyrimidines, and pyrazolopyrimidines were reported. Most of the triazolopyrimidines showed anticonvulsive activity in the maximal electroshock (MES) and pentetrazol (PTZ)-induced seizure models. The compound 6d, holding a median effective dose (ED50) of 15.8 and 14.1 mg/kg against MES and PTZ-induced seizures, respectively, was found to be the most potent one. The protection index (PI) value of 6d was significantly higher than that of some available AEDs. Moreover, the experimental investigation of compound 6d’s mechanism of action suggested that compound 6d works as an anticonvulsant agent by regulating the GABA function. Ullah et al. summarized backbone and/or functionalized fluorinated 1,2,3and 1,2,4triazoles with anticancer, antibacterial, antifungal, antiviral, antimicrobial, herbicidal, inhibitory, antioxidant, antagonistic, antimalarial, and anti-inflammatory properties. It is revealed that many biologically and pharmacologically active fluorine-bearing triazoles have been extensively synthesized by the facile click chemistry approach. Many promising and valuable fluorine-incorporating triazoles’ analogs were reviewed as potential lead candidates for antiviral and anticancer agents. It is conclusion that the development of fluorine-incorporating triazoles toward clinical applications is promising. OPEN ACCESS