摘要
本综述旨在总结大量对称二聚体药物的结构,这些药物具有两种单体,通过桥接实体连接,强调据报道具有二聚体结构的生物活性物质的多功能性。这些化合物的主要数量包括抗癌剂,抗生素/抗微生物药物和抗艾滋病药物。其他对称二聚体药物包括抗糖尿病药,抗抑郁药,镇痛药,抗炎药,治疗阿尔茨海默病的药物,抗胆固醇组学,雌激素,抗氧化剂,酶抑制剂,抗帕金森病,泻药,抗过敏化合物,大麻素等。所审查的大多数文章没有将二聚体的活性/效力与其相应的单体的活性/效力进行比较。只有在有限的情况下,才提出了各种建议来证明二聚体与相应单体相比出乎意料地更高的活性。这些建议包括统计效应,二聚体受体的存在,二聚体同时与两个受体的结合等。几乎不可能预测哪些二聚体比它们各自的单体更可取,或者哪些连接桥将导致最活跃的化合物。预计所提到的物质种类繁多,以及它们生物活性的分类应该引起学术和工业药物化学家的兴趣。
关键词: 单体药物,二聚体药物,对称连接桥梁,协同作用,生物活性,工业化药物化学家。
Current Medicinal Chemistry
Title:Dimeric Drugs
Volume: 29 Issue: 16
关键词: 单体药物,二聚体药物,对称连接桥梁,协同作用,生物活性,工业化药物化学家。
摘要: This review intends to summarize the structures of an extensive number of symmetrical-dimeric drugs, having two monomers, linked via a bridging entity emphasizing the versatility of biologically active substances reported to possess dimeric structures. The major number of these compounds consists of anticancer agents, antibiotics/ antimicrobials, and anti-AIDS drugs. Other symmetrical-dimeric drugs include antidiabetics, antidepressants, analgesics, anti-inflammatories, drugs for the treatment of Alzheimer’s disease, anticholesterolemics, estrogenics, antioxidants, enzyme inhibitors, anti- Parkinsonians, laxatives, antiallergy compounds, cannabinoids, etc. Most of the articles reviewed do not compare the activity/potency of the dimers to that of their corresponding monomers. Only in limited cases, various suggestions have been made to justify the unexpectedly higher activity of the dimers vs. that of the corresponding monomers. These suggestions include statistical effects, the presence of dimeric receptors, binding of a dimer to two receptors simultaneously, and others. It is virtually impossible to predict which dimers will be preferable to their respective monomers, or which linking bridges will lead to the most active compounds. It is expected that the extensive variety of substances mentioned, and the assortment of their biological activities should be of interest to academic and industrial medicinal chemists.
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Cite this article as:
Dimeric Drugs, Current Medicinal Chemistry 2022; 29 (16) . https://dx.doi.org/10.2174/0929867328666210810124159
DOI https://dx.doi.org/10.2174/0929867328666210810124159 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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