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Bioactive pyrrole-based compounds with target selectivity

Authors :
Giovanna Li Petri
Virginia Spanò
Ralph Holl
Alessandra Montalbano
Maria Valeria Raimondi
Roberto Spatola
Paola Barraja
Li Petri Giovanna
Spanò Virginia
Spatola Roberto
Holl Ralph
Raimondi Maria Valeria
Barraja Paola
Montalbano Alessandra
Source :
European Journal of Medicinal Chemistry
Publication Year :
2020
Publisher :
Elsevier BV, 2020.

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.<br />Graphical abstract Image 1<br />Highlights • Pyrrole nucleus is one of the most explored heterocycle in drug discovery. • Pyrrole derivatives exhibit antitumor, antimicrobial and antiviral activities. • Targets involved in their biological activities were identified. • SAR to underline their most important features were discussed.

Details

ISSN :
02235234
Volume :
208
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....54a784a4f066cafb76b019ee931ce7fe