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咪唑类类似物在新药研发中的生物学意义。

Biological Significance of Imidazole-based Analogues in New Drug Development.

机构信息

Faculty of Pharmacy, IFTM University, Moradabad - 244102, India.

Kharvel Subharti College of Pharmacy, Swami Vivekanand Subharti University, Meerut 250005, India.

出版信息

Curr Drug Discov Technol. 2020;17(5):574-584. doi: 10.2174/1570163816666190320123340.

Abstract

In the field of heterocyclic medicinal chemistry, especially five-membered ring structures containing a nitrogen atom, imidazole core is an imperative aromatic heterocycle which is usually present in naturally occurring products and synthetic bioactive molecules. The occurrence of imidazole moiety in therapeutic compounds may be beneficial in terms of improving water-soluble properties due to its two nitrogen atoms which leads to the creation of hydrogen bonds. The imidazole nucleus has also been recognized as an important isostere of triazole, pyrazole, thiazole, tetrazole, oxazole, amide etc. for the purpose of designing and development of various biologically active molecules. Moreover, imidazole core as an attractive binding site could interact with diverse cations and anions as well as biomolecules through different reactions in the human biological system thus displaying extensive biological activities. This effort thoroughly provides a wide-ranging assessment in current drug discovery and developments of imidazolebased analogues in the entire series of synthetic medicinal chemistry as antibacterial and antifungal, anticancer, anti-tubercular, analgesic and anti-inflammatory, anti-neuropathic, antihypertensive, anti-allergic, anti-parasitic, antiviral, antidepressant, anti-obesity and so on, altogether with their prospective approaches in diagnostic and pathological field. It is expected that the present review will be supportive on behalf of new opinions in the search for rational strategies of more efficacious and less toxic medicinal agents and drugs containing imidazole core.

摘要

在杂环药物化学领域,特别是含有氮原子的五元环结构,咪唑核心是一种必不可少的芳香杂环,它通常存在于天然产物和合成生物活性分子中。治疗化合物中咪唑部分的存在可能有利于改善水溶性,因为它的两个氮原子可以形成氢键。咪唑核也被认为是三唑、吡唑、噻唑、四唑、噁唑、酰胺等的重要等排体,用于设计和开发各种具有生物活性的分子。此外,咪唑核心作为一个有吸引力的结合位点,可以通过不同的反应与多种阳离子、阴离子以及生物分子相互作用,从而在人体生物系统中显示出广泛的生物活性。本综述全面评估了咪唑类类似物在整个合成药物化学领域中的药物发现和开发,包括抗菌和抗真菌、抗癌、抗结核、镇痛和抗炎、抗神经病变、抗高血压、抗过敏、抗寄生虫、抗病毒、抗抑郁、抗肥胖等方面的应用,以及它们在诊断和病理领域的潜在应用。预计本综述将为寻找更有效、毒性更低的药物和含有咪唑核心的药物提供新的观点和合理策略提供支持。

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