Cargando…

Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery

Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or...

Descripción completa

Detalles Bibliográficos
Autores principales: Ge, Tony, Cintrat, Jean-Christophe
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8705011/
https://www.ncbi.nlm.nih.gov/pubmed/34959675
http://dx.doi.org/10.3390/ph14121275
_version_ 1784621842385862656
author Ge, Tony
Cintrat, Jean-Christophe
author_facet Ge, Tony
Cintrat, Jean-Christophe
author_sort Ge, Tony
collection PubMed
description Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery.
format Online
Article
Text
id pubmed-8705011
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-87050112021-12-25 Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery Ge, Tony Cintrat, Jean-Christophe Pharmaceuticals (Basel) Review Heterocyclic amino derivatives have been extensively synthesized and validated as potent bioactive compounds, and nowadays, numerous marketed drugs share these scaffolds, from very simple structures (monoamino, monocyclic compounds) to much more complex molecules (polycyclic derivatives with two or more nitrogen atoms within the (fused) rings). In a constant quest for new chemical entities in drug discovery, a few novel heterocycles have emerged in recent years as promising building blocks for the obtainment of bioactive modulators. In this context, pyrrolotriazinones have attracted attention, and some show promising biological activities. Here, we offer an extensive review of pyrrolo[2,1-f][1,2,4]triazin-4(1H)-one and pyrrolo[1,2-d][1,2,4]triazin-4(3H)-one, describing their biological properties en route to drug discovery. MDPI 2021-12-06 /pmc/articles/PMC8705011/ /pubmed/34959675 http://dx.doi.org/10.3390/ph14121275 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
Ge, Tony
Cintrat, Jean-Christophe
Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title_full Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title_fullStr Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title_full_unstemmed Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title_short Pyrrolotriazinone as an Underexplored Scaffold in Drug Discovery
title_sort pyrrolotriazinone as an underexplored scaffold in drug discovery
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8705011/
https://www.ncbi.nlm.nih.gov/pubmed/34959675
http://dx.doi.org/10.3390/ph14121275
work_keys_str_mv AT getony pyrrolotriazinoneasanunderexploredscaffoldindrugdiscovery
AT cintratjeanchristophe pyrrolotriazinoneasanunderexploredscaffoldindrugdiscovery