“噻吩”:含硫杂环作为一种特殊的支架

Ajay Mahaputra Kumar, Yuthika Narayan, Amana Parveen
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引用次数: 0

摘要

在具有有趣治疗特性的杂环化合物的快速扩展的化学领域中,噻吩核已经确立了自己作为一个有前景的实体。通过不同途径产生的可比物质的生物活性大小不同。药物化学家利用他们对多种合成途径和这些化合物的各种物理化学性质的理解来创建一个组合文库,并对铅分子进行彻底的搜索。杂环化合物具有广泛的生物活性,在药物化学中占有重要地位,在药物设计和开发领域得到了广泛的研究。噻吩是一种含硫的杂环支架,作为一种被广泛研究的支架,用于合成具有抗菌、抗精神病、抗癌、镇痛、抗炎、抗心律失常等生物学功能的分子库。根据取代的种类和位置,噻吩类似物已被证明与广泛的癌症特异性蛋白质靶标结合。因此,人们发现噻吩类似物通过抑制各种癌症相关信号通路来发挥其生物学作用。在药物化学中对噻吩的研究产生了将噻吩部分与传统药物成分结合成一个分子的分子。本文综述了含噻吩核化合物的生物和医学活性,以及噻吩的行为、合成和制剂方面的信息,重点介绍了合成技术、生物学概况和构效关系(SAR)研究。
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“Thiophene”: A Sulphur Containing Heterocycle As A Privileged Scaffold
In the rapidly expanding chemical realm of heterocyclic compounds with interesting therapeutic properties, the thiophene nucleus has established itself as a prospective entity. The biological activity of comparable substances produced via different pathways is of varying magnitudes. Medicinal chemists use their understanding of multiple synthetic pathways and the various physicochemical properties of such compounds to create a combinatorial library and conduct thorough searches for lead molecules. Due to their vast spectrum of biological actions, heterocyclic compounds play a crucial role in Medicinal chemistry and are extensively researched in the field of drug design and development. Thiophene, a sulfur-containing heterocyclic scaffold, has emerged as a rather well-explored scaffold for the synthesis of a library of molecules with biological functions, including antibacterial, antipsychotic, anticancer, analgesic, anti-inflammatory, anti-arrhythmic, and so on. Depending on the kind and position of substitution, thiophene analogues have been shown to bind to a wide spectrum of cancer-specific protein targets. As a result, thiophene analogues have been found to exert their biological effects by inhibiting various cancer-related signalling pathways. The study of thiophene in Medicinal chemistry resulted in molecules that combine the thiophene moiety with traditional drug components in a single molecule. This review covers the biological and medical activity of compounds containing a thiophene nucleus, as well as information on thiophene behaviour, synthesis, and agents, with a focus on synthetic techniques, biological profiles, and structure-activity relationship (SAR) research.
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