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The Magic Methyl and Its Tricks in Drug Discovery and Development
One of the key scientific aspects of small-molecule drug discovery and development is the analysis of the relationship between its chemical structure and biological activity. Understanding the effects that lead to significant changes in biological activity is of paramount importance for the rational...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2023
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10457765/ https://www.ncbi.nlm.nih.gov/pubmed/37631072 http://dx.doi.org/10.3390/ph16081157 |
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author | Pinheiro, Pedro de Sena Murteira Franco, Lucas Silva Fraga, Carlos Alberto Manssour |
author_facet | Pinheiro, Pedro de Sena Murteira Franco, Lucas Silva Fraga, Carlos Alberto Manssour |
author_sort | Pinheiro, Pedro de Sena Murteira |
collection | PubMed |
description | One of the key scientific aspects of small-molecule drug discovery and development is the analysis of the relationship between its chemical structure and biological activity. Understanding the effects that lead to significant changes in biological activity is of paramount importance for the rational design and optimization of bioactive molecules. The “methylation effect”, or the “magic methyl” effect, is a factor that stands out due to the number of examples that demonstrate profound changes in either pharmacodynamic or pharmacokinetic properties. In many cases, this has been carried out rationally, but in others it has been the product of serendipitous observations. This paper summarizes recent examples that provide an overview of the current state of the art and contribute to a better understanding of the methylation effect in bioactive small-molecule drug candidates. |
format | Online Article Text |
id | pubmed-10457765 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-104577652023-08-27 The Magic Methyl and Its Tricks in Drug Discovery and Development Pinheiro, Pedro de Sena Murteira Franco, Lucas Silva Fraga, Carlos Alberto Manssour Pharmaceuticals (Basel) Review One of the key scientific aspects of small-molecule drug discovery and development is the analysis of the relationship between its chemical structure and biological activity. Understanding the effects that lead to significant changes in biological activity is of paramount importance for the rational design and optimization of bioactive molecules. The “methylation effect”, or the “magic methyl” effect, is a factor that stands out due to the number of examples that demonstrate profound changes in either pharmacodynamic or pharmacokinetic properties. In many cases, this has been carried out rationally, but in others it has been the product of serendipitous observations. This paper summarizes recent examples that provide an overview of the current state of the art and contribute to a better understanding of the methylation effect in bioactive small-molecule drug candidates. MDPI 2023-08-15 /pmc/articles/PMC10457765/ /pubmed/37631072 http://dx.doi.org/10.3390/ph16081157 Text en © 2023 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 Pinheiro, Pedro de Sena Murteira Franco, Lucas Silva Fraga, Carlos Alberto Manssour The Magic Methyl and Its Tricks in Drug Discovery and Development |
title | The Magic Methyl and Its Tricks in Drug Discovery and Development |
title_full | The Magic Methyl and Its Tricks in Drug Discovery and Development |
title_fullStr | The Magic Methyl and Its Tricks in Drug Discovery and Development |
title_full_unstemmed | The Magic Methyl and Its Tricks in Drug Discovery and Development |
title_short | The Magic Methyl and Its Tricks in Drug Discovery and Development |
title_sort | magic methyl and its tricks in drug discovery and development |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10457765/ https://www.ncbi.nlm.nih.gov/pubmed/37631072 http://dx.doi.org/10.3390/ph16081157 |
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