4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents.
- Publisher:
- MDPI
- Publication Type:
- Journal Article
- Citation:
- Molecules, 2024, 29, (7), pp. 1519
- Issue Date:
- 2024-03-28
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Full metadata record
Field | Value | Language |
---|---|---|
dc.contributor.author | Phillips, MJA | |
dc.contributor.author | Huston, WM | |
dc.contributor.author | McDonagh, AM | |
dc.contributor.author |
Rawling, T https://orcid.org/0000-0002-6624-6586 |
|
dc.date.accessioned | 2024-08-02T02:42:03Z | |
dc.date.available | 2024-03-26 | |
dc.date.available | 2024-08-02T02:42:03Z | |
dc.date.issued | 2024-03-28 | |
dc.identifier.citation | Molecules, 2024, 29, (7), pp. 1519 | |
dc.identifier.issn | 1420-3049 | |
dc.identifier.issn | 1420-3049 | |
dc.identifier.uri | http://hdl.handle.net/10453/179994 | |
dc.description.abstract | 4-Chloroisocoumarin compounds have broad inhibitory properties against serine proteases. Here, we show that selected 3-alkoxy-4-chloroisocoumarins preferentially inhibit the activity of the conserved serine protease High-temperature requirement A of Chlamydia trachomatis. The synthesis of a new series of isocoumarin-based scaffolds has been developed, and their anti-chlamydial properties were investigated. The structure of the alkoxy substituent was found to influence the potency of the compounds against High-temperature requirement A, and modifications to the C-7 position of the 3-alkoxy-4-chloroisocoumarin structure attenuate anti-chlamydial properties. | |
dc.format | Electronic | |
dc.language | eng | |
dc.publisher | MDPI | |
dc.relation.ispartof | Molecules | |
dc.relation.isbasedon | 10.3390/molecules29071519 | |
dc.rights | info:eu-repo/semantics/openAccess | |
dc.subject | 0304 Medicinal and Biomolecular Chemistry, 0305 Organic Chemistry, 0307 Theoretical and Computational Chemistry | |
dc.subject.classification | Organic Chemistry | |
dc.subject.classification | 3404 Medicinal and biomolecular chemistry | |
dc.subject.classification | 3405 Organic chemistry | |
dc.subject.mesh | Protease Inhibitors | |
dc.subject.mesh | Chlamydia trachomatis | |
dc.subject.mesh | Enzyme Therapy | |
dc.subject.mesh | Isocoumarins | |
dc.subject.mesh | Serine Endopeptidases | |
dc.subject.mesh | Serine Proteases | |
dc.subject.mesh | Alcohols | |
dc.subject.mesh | Chlamydia trachomatis | |
dc.subject.mesh | Alcohols | |
dc.subject.mesh | Serine Endopeptidases | |
dc.subject.mesh | Protease Inhibitors | |
dc.subject.mesh | Isocoumarins | |
dc.subject.mesh | Serine Proteases | |
dc.subject.mesh | Enzyme Therapy | |
dc.subject.mesh | Protease Inhibitors | |
dc.subject.mesh | Chlamydia trachomatis | |
dc.subject.mesh | Enzyme Therapy | |
dc.subject.mesh | Isocoumarins | |
dc.subject.mesh | Serine Endopeptidases | |
dc.subject.mesh | Serine Proteases | |
dc.subject.mesh | Alcohols | |
dc.title | 4-Chloroisocoumarins as Chlamydial Protease Inhibitors and Anti-Chlamydial Agents. | |
dc.type | Journal Article | |
utslib.citation.volume | 29 | |
utslib.location.activity | Switzerland | |
utslib.for | 0304 Medicinal and Biomolecular Chemistry | |
utslib.for | 0305 Organic Chemistry | |
utslib.for | 0307 Theoretical and Computational Chemistry | |
pubs.organisational-group | University of Technology Sydney | |
pubs.organisational-group | University of Technology Sydney/Faculty of Science | |
pubs.organisational-group | University of Technology Sydney/Faculty of Science/School of Mathematical and Physical Sciences | |
pubs.organisational-group | University of Technology Sydney/Strength - CCET - Centre for Clean Energy Technology | |
utslib.copyright.status | open_access | * |
dc.rights.license | This work is licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0). To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/ | |
dc.date.updated | 2024-08-02T02:41:58Z | |
pubs.issue | 7 | |
pubs.publication-status | Published online | |
pubs.volume | 29 | |
utslib.citation.issue | 7 |
Abstract:
4-Chloroisocoumarin compounds have broad inhibitory properties against serine proteases. Here, we show that selected 3-alkoxy-4-chloroisocoumarins preferentially inhibit the activity of the conserved serine protease High-temperature requirement A of Chlamydia trachomatis. The synthesis of a new series of isocoumarin-based scaffolds has been developed, and their anti-chlamydial properties were investigated. The structure of the alkoxy substituent was found to influence the potency of the compounds against High-temperature requirement A, and modifications to the C-7 position of the 3-alkoxy-4-chloroisocoumarin structure attenuate anti-chlamydial properties.
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