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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...

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Autores principales: Elsharabasy, Fatma S., Gomha, Sobhi M., Farghaly, Thoraya A., Elzahabi, Heba S. A.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
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.
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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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