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三氮唑:近期发展和生物活性的宝贵见解。

Triazoles: a valuable insight into recent developments and biological activities.

机构信息

Institute of Professional Studies College of Pharmacy, Gwalior 474001, India.

Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra 835215, India.

出版信息

Chin J Nat Med. 2013 Sep;11(5):456-65. doi: 10.1016/S1875-5364(13)60084-9.

Abstract

In recent years, heterocyclic compounds, analogs, and derivatives have attracted strong interest due to their useful biological and pharmacological properties. The small and simple triazole nucleus is present in compounds aimed at evaluating new entities that possess anti-microbial, anti-tumor, antitubercular, anti-convulsant, anti-depressant, antimalarial, and anti-inflammatory activities. Triazoles display a broad range of biological activities and are found in many potent, biologically active compounds, such as trazodone (antidepressant drug), rizatriptan (antimigrane drug), hexaconazole (antifungal drug) and alprazolam (hyptonic, sedative and tranquilizer drug). So far, modifications of the triazole ring have proven highly effective with improved potency and lesser toxicity. The present review highlights the recently synthesized triazoles possessing important biological activities.

摘要

近年来,由于具有有用的生物和药理学性质,杂环化合物、类似物和衍生物引起了强烈的兴趣。小分子且简单的三唑核存在于旨在评估具有抗微生物、抗肿瘤、抗结核、抗惊厥、抗抑郁、抗疟疾和抗炎活性的新实体的化合物中。三唑类化合物具有广泛的生物活性,并且存在于许多有效的生物活性化合物中,如曲唑酮(抗抑郁药)、利扎曲坦(抗偏头痛药)、己康唑(抗真菌药)和阿普唑仑(抗高血压药、镇静剂和安定药)。到目前为止,三唑环的修饰已被证明具有非常高的效果,提高了效力,降低了毒性。本综述重点介绍了最近合成的具有重要生物活性的三唑类化合物。

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