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A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()

Ureases are enzymes that hydrolyze urea into ammonium and carbon dioxide. They have received considerable attention due to their impacts on living organism health, since the urease activity in microorganisms, particularly in bacteria, are potential causes and/or factors contributing to the persisten...

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Autores principales: Rego, Yuri F., Queiroz, Marcelo P., Brito, Tiago O., Carvalho, Priscila G., de Queiroz, Vagner T., de Fátima, Ângelo, Macedo Jr., Fernando
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6077150/
https://www.ncbi.nlm.nih.gov/pubmed/30094084
http://dx.doi.org/10.1016/j.jare.2018.05.003
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author Rego, Yuri F.
Queiroz, Marcelo P.
Brito, Tiago O.
Carvalho, Priscila G.
de Queiroz, Vagner T.
de Fátima, Ângelo
Macedo Jr., Fernando
author_facet Rego, Yuri F.
Queiroz, Marcelo P.
Brito, Tiago O.
Carvalho, Priscila G.
de Queiroz, Vagner T.
de Fátima, Ângelo
Macedo Jr., Fernando
author_sort Rego, Yuri F.
collection PubMed
description Ureases are enzymes that hydrolyze urea into ammonium and carbon dioxide. They have received considerable attention due to their impacts on living organism health, since the urease activity in microorganisms, particularly in bacteria, are potential causes and/or factors contributing to the persistence of some pathogen infections. This review compiles examples of the most potent antiurease organic substances. Emphasis was given to systematic screening studies on the inhibitory activity of rationally designed series of compounds with the corresponding SAR considerations. Ureases of Canavalia ensiformis, the usual model in antiureolytic studies, are emphasized. Although the active site of this class of hydrolases is conserved among bacteria and vegetal ureases, the same is not observerd for allosteric site. Therefore, inhibitors acting by participating in interactions with the allosteric site are more susceptible to a potential lack of association among their inhibitory profile for different ureases. The information about the inhibitory activity of different classes of compounds can be usefull to guide the development of new urease inhibitors that may be used in future in small molecular therapy against pathogenic bacteria.
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spelling pubmed-60771502018-08-09 A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria() Rego, Yuri F. Queiroz, Marcelo P. Brito, Tiago O. Carvalho, Priscila G. de Queiroz, Vagner T. de Fátima, Ângelo Macedo Jr., Fernando J Adv Res Article Ureases are enzymes that hydrolyze urea into ammonium and carbon dioxide. They have received considerable attention due to their impacts on living organism health, since the urease activity in microorganisms, particularly in bacteria, are potential causes and/or factors contributing to the persistence of some pathogen infections. This review compiles examples of the most potent antiurease organic substances. Emphasis was given to systematic screening studies on the inhibitory activity of rationally designed series of compounds with the corresponding SAR considerations. Ureases of Canavalia ensiformis, the usual model in antiureolytic studies, are emphasized. Although the active site of this class of hydrolases is conserved among bacteria and vegetal ureases, the same is not observerd for allosteric site. Therefore, inhibitors acting by participating in interactions with the allosteric site are more susceptible to a potential lack of association among their inhibitory profile for different ureases. The information about the inhibitory activity of different classes of compounds can be usefull to guide the development of new urease inhibitors that may be used in future in small molecular therapy against pathogenic bacteria. Elsevier 2018-05-04 /pmc/articles/PMC6077150/ /pubmed/30094084 http://dx.doi.org/10.1016/j.jare.2018.05.003 Text en © 2018 Production and hosting by Elsevier B.V. on behalf of Cairo University. http://creativecommons.org/licenses/by-nc-nd/4.0/ This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Article
Rego, Yuri F.
Queiroz, Marcelo P.
Brito, Tiago O.
Carvalho, Priscila G.
de Queiroz, Vagner T.
de Fátima, Ângelo
Macedo Jr., Fernando
A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title_full A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title_fullStr A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title_full_unstemmed A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title_short A review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
title_sort review on the development of urease inhibitors as antimicrobial agents against pathogenic bacteria()
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6077150/
https://www.ncbi.nlm.nih.gov/pubmed/30094084
http://dx.doi.org/10.1016/j.jare.2018.05.003
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