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1,2,4-Triazole A Privileged Scaffold For The Development Of Potent Antifungal Agents-A Brief Review.
Current Topics in Medicinal Chemistry ( IF 2.9 ) Pub Date : 2020-08-31 , DOI: 10.2174/1568026620666200704140107
Christophe Tratrat 1
Affiliation  

Over the past decades, a tremendous rise in invasive fungal infection diseases attributed to the yeast Candida albicans in immunocompromised individuals poses a seriously challenging issue. Another concern is the emergence of multi-drug resistant pathogens to the existing medicines due to their overuse and misuse. It was recently reported that 25-55% of the mortality rate is caused by invasive infection. Despite a large variety of drugs being available to treat invasive candidiasis, only two of them contain a 1,2,4-triazole core, namely Fluconazole and itraconazole, which are efficient in treating infection induced by fungal Candida species. Moreover, long-term therapy associated with azole medications has led to an increase in azole resistance as well as a high risk of toxicity. Despite numerous outstanding achievements in antifungal drug discovery, development of novel, safer and potent antifungal agents while overcoming the resistance problem associated with the current drugs is becoming the main focus of medicinal chemists. Therefore, this review outlines the breakthroughs in medicinal chemistry research regarding 1,2,4- triazole-based derivatives as potential antifungal agents in the past decade. In addition, the structureactivity relationship of these compounds is also discussed.



中文翻译:

1,2,4-三唑A特权支架,用于开发有效的抗真菌剂-简要评述。

在过去的几十年中,在免疫受损的个体中归因于白色念珠菌的侵袭性真菌感染疾病的急剧增加构成了一个严重的挑战性问题。另一个令人担忧的问题是,由于过度使用和滥用,对现有药物产生了多重耐药性病原体。最近报道,死亡率的25-55%是由侵入性感染引起的。尽管有多种药物可用于治疗侵袭性念珠菌病,但其中只有两种含有1,2,4-三唑核心,即氟康唑和伊曲康唑,它们可有效治疗由真菌念珠菌引起的感染。此外,与唑类药物相关的长期治疗已导致唑类耐药性增加以及毒性高风险。尽管在抗真菌药物的发现方面取得了许多杰出的成就,但是在克服与现有药物有关的耐药性问题的同时,开发新型,更安全和有效的抗真菌剂已成为药物化学家的主要重点。因此,本综述概述了在过去十年中有关1,2,4-三唑基衍生物作为潜在抗真菌剂的药物化学研究的突破。另外,还讨论了这些化合物的结构活性关系。在过去的十年中,基于4-三唑的衍生物作为潜在的抗真菌剂。此外,还讨论了这些化合物的结构活性关系。在过去的十年中,基于4-三唑的衍生物作为潜在的抗真菌剂。另外,还讨论了这些化合物的结构活性关系。

更新日期:2020-11-02
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