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Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition

Human neutrophil elastase (HNE) and proteinase 3 (Pr3) released from neutrophils at inflammatory sites are the major causes of pathogens in chronic obstructive pulmonary disease (COPD) and various lung tissue derangements, among which cystic fibrosis and blockade of airway passages are chronic. Thes...

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Autores principales: S., Meena, S., Jubie, C., Pramila, A., Manal T. N., S., Gigi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10107027/
https://www.ncbi.nlm.nih.gov/pubmed/37077993
http://dx.doi.org/10.1039/d3ra00106g
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author S., Meena
S., Jubie
C., Pramila
A., Manal T. N.
S., Gigi
author_facet S., Meena
S., Jubie
C., Pramila
A., Manal T. N.
S., Gigi
author_sort S., Meena
collection PubMed
description Human neutrophil elastase (HNE) and proteinase 3 (Pr3) released from neutrophils at inflammatory sites are the major causes of pathogens in chronic obstructive pulmonary disease (COPD) and various lung tissue derangements, among which cystic fibrosis and blockade of airway passages are chronic. These proteolytic mediatory agents combined with induced oxidative reactions sustain pathogenicity. Cyclic diketone indane-1,3-dione derivatives were designed, and toxicity evaluation predictions were performed in silico. Benzimidazole and hydrazide derivatives of indanedione were synthesized and characterized. Synthesized compounds were run using neutrophil elastase inhibition assay protocols. The compounds exhibit considerable inhibition of neutrophil elastase enzymes.
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spelling pubmed-101070272023-04-18 Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition S., Meena S., Jubie C., Pramila A., Manal T. N. S., Gigi RSC Adv Chemistry Human neutrophil elastase (HNE) and proteinase 3 (Pr3) released from neutrophils at inflammatory sites are the major causes of pathogens in chronic obstructive pulmonary disease (COPD) and various lung tissue derangements, among which cystic fibrosis and blockade of airway passages are chronic. These proteolytic mediatory agents combined with induced oxidative reactions sustain pathogenicity. Cyclic diketone indane-1,3-dione derivatives were designed, and toxicity evaluation predictions were performed in silico. Benzimidazole and hydrazide derivatives of indanedione were synthesized and characterized. Synthesized compounds were run using neutrophil elastase inhibition assay protocols. The compounds exhibit considerable inhibition of neutrophil elastase enzymes. The Royal Society of Chemistry 2023-04-17 /pmc/articles/PMC10107027/ /pubmed/37077993 http://dx.doi.org/10.1039/d3ra00106g Text en This journal is © The Royal Society of Chemistry https://creativecommons.org/licenses/by-nc/3.0/
spellingShingle Chemistry
S., Meena
S., Jubie
C., Pramila
A., Manal T. N.
S., Gigi
Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title_full Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title_fullStr Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title_full_unstemmed Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title_short Synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
title_sort synthesis and screening of cyclic diketone indanedione derivatives as future scaffolds for neutrophil elastase inhibition
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10107027/
https://www.ncbi.nlm.nih.gov/pubmed/37077993
http://dx.doi.org/10.1039/d3ra00106g
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