Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives

A series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The com...

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Main Authors: Fareed Ghulam, Afza Nighat, Versiani Ali Muhammad, Fareed Nazia, Mughal Rasheed Uzma, Kalhoro Ali Mahboob, Iqbal Lubna, Lateef Mehreen
Format: Article
Language:English
Published: Serbian Chemical Society 2013-01-01
Series:Journal of the Serbian Chemical Society
Subjects:
Online Access:http://www.doiserbia.nb.rs/img/doi/0352-5139/2013/0352-51391200126F.pdf
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author Fareed Ghulam
Afza Nighat
Versiani Ali Muhammad
Fareed Nazia
Mughal Rasheed Uzma
Kalhoro Ali Mahboob
Iqbal Lubna
Lateef Mehreen
author_facet Fareed Ghulam
Afza Nighat
Versiani Ali Muhammad
Fareed Nazia
Mughal Rasheed Uzma
Kalhoro Ali Mahboob
Iqbal Lubna
Lateef Mehreen
author_sort Fareed Ghulam
collection DOAJ
description A series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The compounds (2-6) are new derivatives. The structures of compounds were evaluated on the basis of 1H-NMR, 13C-NMR, EIMS, FT-IR and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. Antibacterial activity was tested by agar well diffusion method using Mueller Hinton Agar medium. Compound (2) showed excellent activity against S. aureus which has 16 mm (80%) inhibition and above 24 mm (70%) against S. typhi. The most active compound against E. coli was compound (6) having 20 mm (80%) inhibition followed by compound (5) having above 18 mm (70%) inhibition. Urease inhibition activity of all the compounds was determined by indophenol method. Compounds (3, 6) and (7) showed significant inhibition against Jacks bean urease.
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spelling doaj.art-37213e9db79d4cdaa7c9ba31817a615a2022-12-21T18:51:39ZengSerbian Chemical SocietyJournal of the Serbian Chemical Society0352-51392013-01-017881127113410.2298/JSC120917126FSynthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivativesFareed GhulamAfza NighatVersiani Ali MuhammadFareed NaziaMughal Rasheed UzmaKalhoro Ali MahboobIqbal LubnaLateef MehreenA series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The compounds (2-6) are new derivatives. The structures of compounds were evaluated on the basis of 1H-NMR, 13C-NMR, EIMS, FT-IR and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. Antibacterial activity was tested by agar well diffusion method using Mueller Hinton Agar medium. Compound (2) showed excellent activity against S. aureus which has 16 mm (80%) inhibition and above 24 mm (70%) against S. typhi. The most active compound against E. coli was compound (6) having 20 mm (80%) inhibition followed by compound (5) having above 18 mm (70%) inhibition. Urease inhibition activity of all the compounds was determined by indophenol method. Compounds (3, 6) and (7) showed significant inhibition against Jacks bean urease.http://www.doiserbia.nb.rs/img/doi/0352-5139/2013/0352-51391200126F.pdfaldehydeantibacterialUrease inhibition activitiesoxazolonessynthesiszinc Oxide (ZnO)
spellingShingle Fareed Ghulam
Afza Nighat
Versiani Ali Muhammad
Fareed Nazia
Mughal Rasheed Uzma
Kalhoro Ali Mahboob
Iqbal Lubna
Lateef Mehreen
Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
Journal of the Serbian Chemical Society
aldehyde
antibacterial
Urease inhibition activities
oxazolones
synthesis
zinc Oxide (ZnO)
title Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
title_full Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
title_fullStr Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
title_full_unstemmed Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
title_short Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
title_sort synthesis spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
topic aldehyde
antibacterial
Urease inhibition activities
oxazolones
synthesis
zinc Oxide (ZnO)
url http://www.doiserbia.nb.rs/img/doi/0352-5139/2013/0352-51391200126F.pdf
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