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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...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society of Chemistry
2023
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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. |
format | Online Article Text |
id | pubmed-10107027 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2023 |
publisher | The Royal Society of Chemistry |
record_format | MEDLINE/PubMed |
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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