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药物化学与药物设计中的曼尼希碱

Mannich bases in medicinal chemistry and drug design.

作者信息

Roman Gheorghe

机构信息

Petru Poni Institute of Macromolecular Chemistry, Department of Inorganic Polymers, 41A Aleea Gr. Ghica Vodă, Iaşi 700487, Romania.

出版信息

Eur J Med Chem. 2015 Jan 7;89:743-816. doi: 10.1016/j.ejmech.2014.10.076. Epub 2014 Oct 30.

DOI:10.1016/j.ejmech.2014.10.076
PMID:25462280
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7115492/
Abstract

The biological activity of Mannich bases, a structurally heterogeneous class of chemical compounds that are generated from various substrates through the introduction of an aminomethyl function by means of the Mannich reaction, is surveyed, with emphasis on the relationship between structure and biological activity. The review covers extensively the literature reports that have disclosed Mannich bases as anticancer and cytotoxic agents, or compounds with potential antibacterial and antifungal activity in the last decade. The most relevant studies on the activity of Mannich bases as antimycobacterial agents, antimalarials, or antiviral candidates have been included as well. The review contains also a thorough coverage of anticonvulsant, anti-inflammatory, analgesic and antioxidant activities of Mannich bases. In addition, several minor biological activities of Mannich bases, such as their ability to regulate blood pressure or inhibit platelet aggregation, their antiparasitic and anti-ulcer effects, as well as their use as agents for the treatment of mental disorders have been presented. The review gives in the end a brief overview of the potential of Mannich bases as inhibitors of various enzymes or ligands for several receptors.

摘要

本文综述了曼尼希碱的生物活性,这是一类结构各异的化合物,通过曼尼希反应引入氨甲基官能团,由各种底物生成,重点是结构与生物活性之间的关系。本综述广泛涵盖了过去十年中已披露曼尼希碱作为抗癌和细胞毒性剂,或具有潜在抗菌和抗真菌活性的化合物的文献报道。还纳入了关于曼尼希碱作为抗分枝杆菌剂、抗疟药或抗病毒候选物活性的最相关研究。该综述还全面涵盖了曼尼希碱的抗惊厥、抗炎、镇痛和抗氧化活性。此外,还介绍了曼尼希碱的几种次要生物活性,例如它们调节血压或抑制血小板聚集的能力、抗寄生虫和抗溃疡作用,以及它们作为治疗精神障碍药物的用途。该综述最后简要概述了曼尼希碱作为各种酶抑制剂或几种受体配体的潜力。

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