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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Main Authors: Fatma S. Elsharabasy, Sobhi M. Gomha, Thoraya A. Farghaly, Heba S. A. Elzahabi
Format: Article
Language:English
Published: MDPI AG 2017-02-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/22/2/319
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author Fatma S. Elsharabasy
Sobhi M. Gomha
Thoraya A. Farghaly
Heba S. A. Elzahabi
author_facet Fatma S. Elsharabasy
Sobhi M. Gomha
Thoraya A. Farghaly
Heba S. A. Elzahabi
author_sort Fatma S. Elsharabasy
collection DOAJ
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 doaj.art-b0396daabfb44fc7975b66b20bf63e3b2022-12-22T02:53:45ZengMDPI AGMolecules1420-30492017-02-0122231910.3390/molecules22020319molecules22020319An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound IrradiationFatma S. Elsharabasy0Sobhi M. Gomha1Thoraya A. Farghaly2Heba S. A. Elzahabi3Department of Chemistry of Natural and Microbial Products, National Research Center, Dokki 12622, EgyptDepartment of Chemistry, Faculty of Science, Cairo University, Giza 12613, EgyptDepartment of Chemistry, Faculty of Science, Cairo University, Giza 12613, EgyptDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy (Girls), AlAzhar University, Cairo1 1754, EgyptNovel 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.http://www.mdpi.com/1420-3049/22/2/319thiazolylphthalazinedioneshydrazonoyl chloridesultrasound irradiationantimicrobial activity
spellingShingle Fatma S. Elsharabasy
Sobhi M. Gomha
Thoraya A. Farghaly
Heba S. A. Elzahabi
An Efficient Synthesis of Novel Bioactive Thiazolyl-Phthalazinediones under Ultrasound Irradiation
Molecules
thiazolylphthalazinediones
hydrazonoyl chlorides
ultrasound irradiation
antimicrobial activity
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 thiazolylphthalazinediones
hydrazonoyl chlorides
ultrasound irradiation
antimicrobial activity
url http://www.mdpi.com/1420-3049/22/2/319
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