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Bioactive pyrrole-based compounds with target selectivity.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-08-29 , DOI: 10.1016/j.ejmech.2020.112783
Giovanna Li Petri 1 , Virginia Spanò 1 , Roberto Spatola 1 , Ralph Holl 2 , Maria Valeria Raimondi 1 , Paola Barraja 1 , Alessandra Montalbano 1
Affiliation  

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.



中文翻译:

具有目标选择性的基于生物活性吡咯的化合物。

具有药物样性质的新型合成化合物的发现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-杂环基序。其中,吡咯环是药物发现计划中几个治疗领域中研究最多的杂环之一,这已得到市场上大量基于吡咯的药物的证实。在本综述中,我们重点研究了2015年至2019年间文献中报道的吡咯及其具有抗癌,抗微生物和抗病毒活性的杂种融合衍生物,其中确定了一个特定目标以负责其生物学活性。结果表明,作为许多药物的药效团单元的吡咯核所提供的强大的药物学和药理学特征仍被药物化学家所认可。

更新日期:2020-09-10
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