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Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents

Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective pr...

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Detalles Bibliográficos
Autores principales: Lagardère, Prisca, Fersing, Cyril, Masurier, Nicolas, Lisowski, Vincent
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8780093/
https://www.ncbi.nlm.nih.gov/pubmed/35056092
http://dx.doi.org/10.3390/ph15010035
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author Lagardère, Prisca
Fersing, Cyril
Masurier, Nicolas
Lisowski, Vincent
author_facet Lagardère, Prisca
Fersing, Cyril
Masurier, Nicolas
Lisowski, Vincent
author_sort Lagardère, Prisca
collection PubMed
description Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective properties. Broad-spectrum thienopyrimidines with biological properties such as antibacterial, antifungal, antiparasitic and antiviral inspired us to analyze and compile their structure–activity relationship (SAR) and classify their synthetic pathways. This review explains the main access route to synthesize thienopyrimidines from thiophene derivatives or from pyrimidine analogs. In addition, SAR study and promising anti-infective activity of these scaffolds are summarized in figures and explanatory diagrams. Ligand–receptor interactions were modeled when the biological target was identified and the crystal structure was solved.
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spelling pubmed-87800932022-01-22 Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents Lagardère, Prisca Fersing, Cyril Masurier, Nicolas Lisowski, Vincent Pharmaceuticals (Basel) Review Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective properties. Broad-spectrum thienopyrimidines with biological properties such as antibacterial, antifungal, antiparasitic and antiviral inspired us to analyze and compile their structure–activity relationship (SAR) and classify their synthetic pathways. This review explains the main access route to synthesize thienopyrimidines from thiophene derivatives or from pyrimidine analogs. In addition, SAR study and promising anti-infective activity of these scaffolds are summarized in figures and explanatory diagrams. Ligand–receptor interactions were modeled when the biological target was identified and the crystal structure was solved. MDPI 2021-12-27 /pmc/articles/PMC8780093/ /pubmed/35056092 http://dx.doi.org/10.3390/ph15010035 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Lagardère, Prisca
Fersing, Cyril
Masurier, Nicolas
Lisowski, Vincent
Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title_full Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title_fullStr Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title_full_unstemmed Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title_short Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents
title_sort thienopyrimidine: a promising scaffold to access anti-infective agents
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8780093/
https://www.ncbi.nlm.nih.gov/pubmed/35056092
http://dx.doi.org/10.3390/ph15010035
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