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An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation
Novel 2-thiazolylphthalazine derivatives were efficiently synthesized under ultrasound irradiation, resulting in high yields and short reaction times after optimization of the reaction conditions. All prepared compounds were fully characterized using spectroscopic methods. They were screened for the...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155881/ https://www.ncbi.nlm.nih.gov/pubmed/28218718 http://dx.doi.org/10.3390/molecules22020319 |
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author | Elsharabasy, Fatma S. Gomha, Sobhi M. Farghaly, Thoraya A. Elzahabi, Heba S. A. |
author_facet | Elsharabasy, Fatma S. Gomha, Sobhi M. Farghaly, Thoraya A. Elzahabi, Heba S. A. |
author_sort | Elsharabasy, Fatma S. |
collection | PubMed |
description | Novel 2-thiazolylphthalazine derivatives were efficiently synthesized under ultrasound irradiation, resulting in high yields and short reaction times after optimization of the reaction conditions. All prepared compounds were fully characterized using spectroscopic methods. They were screened for their antimicrobial activity against Gram-positive and Gram-negative bacteria as well as for antifungal activity. The antimicrobial activity profile of the tested compounds showed some promising results. The potent activity of compounds 4d, 7b (117% zone inhibition) and 7c (105% zone inhibition) against Salmonella sp., exceeding that of the reference drug Gentamycin is particularly noteworthy. In general, the newly synthesized thiazolylphthalazine derivatives showed higher antimicrobial activity against the tested Gram-negative bacteria than against Gram-positive bacteria and fungi. |
format | Online Article Text |
id | pubmed-6155881 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61558812018-11-13 An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation Elsharabasy, Fatma S. Gomha, Sobhi M. Farghaly, Thoraya A. Elzahabi, Heba S. A. Molecules Article Novel 2-thiazolylphthalazine derivatives were efficiently synthesized under ultrasound irradiation, resulting in high yields and short reaction times after optimization of the reaction conditions. All prepared compounds were fully characterized using spectroscopic methods. They were screened for their antimicrobial activity against Gram-positive and Gram-negative bacteria as well as for antifungal activity. The antimicrobial activity profile of the tested compounds showed some promising results. The potent activity of compounds 4d, 7b (117% zone inhibition) and 7c (105% zone inhibition) against Salmonella sp., exceeding that of the reference drug Gentamycin is particularly noteworthy. In general, the newly synthesized thiazolylphthalazine derivatives showed higher antimicrobial activity against the tested Gram-negative bacteria than against Gram-positive bacteria and fungi. MDPI 2017-02-18 /pmc/articles/PMC6155881/ /pubmed/28218718 http://dx.doi.org/10.3390/molecules22020319 Text en © 2017 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Elsharabasy, Fatma S. Gomha, Sobhi M. Farghaly, Thoraya A. Elzahabi, Heba S. A. An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title | An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title_full | An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title_fullStr | An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title_full_unstemmed | An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title_short | An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation |
title_sort | efficient synthesis of novel bioactive thiazolyl-phthalazinediones under ultrasound irradiation |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155881/ https://www.ncbi.nlm.nih.gov/pubmed/28218718 http://dx.doi.org/10.3390/molecules22020319 |
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