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Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives
Herein, we report the obtaining of new hybrid molecules of amphetamine with different profens (amfens). The obtained amfens are characterized by their melting points, UV, (1)H–, (13)C–NMR, and HRMS spectra. A complete and detailed mass spectral analysis of the newly obtained derivatives of amphetami...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9822421/ https://www.ncbi.nlm.nih.gov/pubmed/36615344 http://dx.doi.org/10.3390/molecules28010151 |
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author | Manolov, Stanimir Ivanov, Iliyan Bojilov, Dimitar Nedialkov, Paraskev |
author_facet | Manolov, Stanimir Ivanov, Iliyan Bojilov, Dimitar Nedialkov, Paraskev |
author_sort | Manolov, Stanimir |
collection | PubMed |
description | Herein, we report the obtaining of new hybrid molecules of amphetamine with different profens (amfens). The obtained amfens are characterized by their melting points, UV, (1)H–, (13)C–NMR, and HRMS spectra. A complete and detailed mass spectral analysis of the newly obtained derivatives of amphetamine with ibuprofen, flurbiprofen, ketoprofen, naproxen, and carprofen was performed. In vitro inhibition of albumin denaturation of each new compound was assessed, and they showed significant activity. The IC(50) values of the obtained amphetamine-profen derivatives ranged from 92.81 to 159.87 µg/mL. This indicates that the new hybrids inherit the anti-inflammatory properties of profens. Using in silico method, the toxicity was also calculated. The obtained results are given in LD(50) values. Depending on the route of administration, the amfens are less toxic compared to the standard amphetamine. |
format | Online Article Text |
id | pubmed-9822421 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-98224212023-01-07 Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives Manolov, Stanimir Ivanov, Iliyan Bojilov, Dimitar Nedialkov, Paraskev Molecules Article Herein, we report the obtaining of new hybrid molecules of amphetamine with different profens (amfens). The obtained amfens are characterized by their melting points, UV, (1)H–, (13)C–NMR, and HRMS spectra. A complete and detailed mass spectral analysis of the newly obtained derivatives of amphetamine with ibuprofen, flurbiprofen, ketoprofen, naproxen, and carprofen was performed. In vitro inhibition of albumin denaturation of each new compound was assessed, and they showed significant activity. The IC(50) values of the obtained amphetamine-profen derivatives ranged from 92.81 to 159.87 µg/mL. This indicates that the new hybrids inherit the anti-inflammatory properties of profens. Using in silico method, the toxicity was also calculated. The obtained results are given in LD(50) values. Depending on the route of administration, the amfens are less toxic compared to the standard amphetamine. MDPI 2022-12-24 /pmc/articles/PMC9822421/ /pubmed/36615344 http://dx.doi.org/10.3390/molecules28010151 Text en © 2022 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 | Article Manolov, Stanimir Ivanov, Iliyan Bojilov, Dimitar Nedialkov, Paraskev Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title | Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title_full | Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title_fullStr | Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title_full_unstemmed | Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title_short | Synthesis, In Vitro Anti-Inflammatory Activity, and HRMS Analysis of New Amphetamine Derivatives |
title_sort | synthesis, in vitro anti-inflammatory activity, and hrms analysis of new amphetamine derivatives |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9822421/ https://www.ncbi.nlm.nih.gov/pubmed/36615344 http://dx.doi.org/10.3390/molecules28010151 |
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