Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , , , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Brazilian Journal of Pharmaceutical Sciences |
Texto Completo: | https://www.revistas.usp.br/bjps/article/view/181919 |
Resumo: | The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively. |
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Brazilian Journal of Pharmaceutical Sciences |
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Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives4-HydroxycoumarinAnti-ureaseCarbonic anhydraseAldehydesAntibacterialThe 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2021-03-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/18191910.1590/s2175-97902019000418654Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18654 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18654 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18654 2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/181919/168755Copyright (c) 2020 Brazilian Journal of Pharmaceutical Scienceshttp://creativecommons.org/licenses/by/4.0info:eu-repo/semantics/openAccessSaleem, Afia Bukhari, Syed Majid Zaidi, Asma Farooq, Umar Ali, Majid Khan, Asma Khan, Sidra Shah, Kausar Hussain Mahmood, Adeem Khan, Farhan Ahmed 2021-06-12T19:46:54Zoai:revistas.usp.br:article/181919Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2021-06-12T19:46:54Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false |
dc.title.none.fl_str_mv |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
title |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
spellingShingle |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives Saleem, Afia 4-Hydroxycoumarin Anti-urease Carbonic anhydrase Aldehydes Antibacterial |
title_short |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
title_full |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
title_fullStr |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
title_full_unstemmed |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
title_sort |
Enzyme inhibition and antibacterial potential of 4-Hydroxycoumarin derivatives |
author |
Saleem, Afia |
author_facet |
Saleem, Afia Bukhari, Syed Majid Zaidi, Asma Farooq, Umar Ali, Majid Khan, Asma Khan, Sidra Shah, Kausar Hussain Mahmood, Adeem Khan, Farhan Ahmed |
author_role |
author |
author2 |
Bukhari, Syed Majid Zaidi, Asma Farooq, Umar Ali, Majid Khan, Asma Khan, Sidra Shah, Kausar Hussain Mahmood, Adeem Khan, Farhan Ahmed |
author2_role |
author author author author author author author author author |
dc.contributor.author.fl_str_mv |
Saleem, Afia Bukhari, Syed Majid Zaidi, Asma Farooq, Umar Ali, Majid Khan, Asma Khan, Sidra Shah, Kausar Hussain Mahmood, Adeem Khan, Farhan Ahmed |
dc.subject.por.fl_str_mv |
4-Hydroxycoumarin Anti-urease Carbonic anhydrase Aldehydes Antibacterial |
topic |
4-Hydroxycoumarin Anti-urease Carbonic anhydrase Aldehydes Antibacterial |
description |
The 4-Hydroxycoumarin derivatives are known to show a broad spectrum of pharmacological applications. In this paper we are reporting the synthesis of a new series of 4-Hydroxycoumarin derivatives synthesized through Knovenegal condensation; they were characterized by using UV-Vis, FT-IR, NMR spectroscopies. The synthesized compounds were evaluated for antibacterial activity against Staphylococcus aureus and Salmonella typhimurium strains. The compounds (2), (3) and (8) showed favorable antibacterial activity with zone of inhibitions 26.5± 0.84, 26.0 ± 0.56 and 26.0 ± 0.26 against Staphylococcus aureus (Gram-positive) respectively. However, the compounds (5) and (9) were found more active with 19.5 ± 0.59 and 19.5 ± 0.32 zone of inhibitions against Salmonella typhimurium (Gram-negative). Whereas, in urease inhibition assay, none of the synthesized derivatives showed significant anti-urease activity; although, in carbonic anhydrase-II inhibition assay, the compound (2) and (6) showed enzyme inhibition activity with IC50 values 263±0.3 and 456±0.1, respectively. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-03-02 |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181919 10.1590/s2175-97902019000418654 |
url |
https://www.revistas.usp.br/bjps/article/view/181919 |
identifier_str_mv |
10.1590/s2175-97902019000418654 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
https://www.revistas.usp.br/bjps/article/view/181919/168755 |
dc.rights.driver.fl_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
Copyright (c) 2020 Brazilian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/4.0 |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
publisher.none.fl_str_mv |
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas |
dc.source.none.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18654 Brazilian Journal of Pharmaceutical Sciences; v. 56 (2020); e18654 Brazilian Journal of Pharmaceutical Sciences; Vol. 56 (2020); e18654 2175-9790 1984-8250 reponame:Brazilian Journal of Pharmaceutical Sciences instname:Universidade de São Paulo (USP) instacron:USP |
instname_str |
Universidade de São Paulo (USP) |
instacron_str |
USP |
institution |
USP |
reponame_str |
Brazilian Journal of Pharmaceutical Sciences |
collection |
Brazilian Journal of Pharmaceutical Sciences |
repository.name.fl_str_mv |
Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP) |
repository.mail.fl_str_mv |
bjps@usp.br||elizabeth.igne@gmail.com |
_version_ |
1800222915166208000 |