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具有目标选择性的生物活性吡咯基化合物。

Bioactive pyrrole-based compounds with target selectivity.

机构信息

Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123, Palermo, Italy.

Department of Chemistry, Institute of Organic Chemistry, University of Hamburg, Martin-Luther-King-Platz 6, 20146, Hamburg, Germany.

出版信息

Eur J Med Chem. 2020 Dec 15;208:112783. doi: 10.1016/j.ejmech.2020.112783. Epub 2020 Aug 29.

Abstract

The discovery of novel synthetic compounds with drug-like properties is an ongoing challenge in medicinal chemistry. Natural products have inspired the synthesis of compounds for pharmaceutical application, most of which are based on N-heterocyclic motifs. Among these, the pyrrole ring is one of the most explored heterocycles in drug discovery programs for several therapeutic areas, confirmed by the high number of pyrrole-based drugs reaching the market. In the present review, we focused on pyrrole and its hetero-fused derivatives with anticancer, antimicrobial, and antiviral activities, reported in the literature between 2015 and 2019, for which a specific target was identified, being responsible for their biological activity. It emerges that the powerful pharmaceutical and pharmacological features provided by the pyrrole nucleus as pharmacophore unit of many drugs are still recognized by medicinal chemists.

摘要

发现具有类药性的新型合成化合物是药物化学中的一个持续挑战。天然产物激发了用于药物应用的化合物的合成,其中大多数基于 N-杂环母核。在这些化合物中,吡咯环是药物发现计划中探索最多的杂环之一,在多个治疗领域中,基于吡咯的药物数量众多,这证实了这一点。在本综述中,我们重点介绍了在 2015 年至 2019 年期间文献中报道的具有抗癌、抗菌和抗病毒活性的吡咯及其杂环稠合衍生物,其中确定了特定的靶标,这些靶标负责其生物活性。事实证明,吡咯核作为许多药物的药效团单元所提供的强大的药物和药理学特性仍然被药物化学家所认可。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4514/7455853/cac860553341/fx1_lrg.jpg

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