dc.contributor.author | Kerda, Marek | |
dc.contributor.author | Šlechta, Petr | |
dc.contributor.author | Janďourek, Ondřej | |
dc.contributor.author | Konečná, Klára | |
dc.contributor.author | Hatoková, Paulína | |
dc.contributor.author | Paterová, Pavla | |
dc.contributor.author | Zitko, Jan | |
dc.date.accessioned | 2024-03-21T12:10:38Z | |
dc.date.available | 2024-03-21T12:10:38Z | |
dc.date.issued | 2023 | |
dc.identifier.uri | https://hdl.handle.net/20.500.14178/2404 | |
dc.description.abstract | Background: The development of novel antimicrobial drugs is an essential part of combatting the uprising of antimicrobial resistance. Proper hit-to-lead development is crucially needed. Methods & results: We present a hit-expansion study of N-pyrazinyl- and N-pyridyl-hydroxybenzamides with a comprehensive determination of structure-activity relationships. The antimicrobial screening revealed high selectivity to staphylococci along with antimycobacterial activity with the best value of 6.25 mu g/ml against Mycobacterium tuberculosis H37Rv. We proved an inhibition of proteosynthesis and a membrane depolarization of methicillin-resistant Staphylococcus aureus. Conclusion: Our results are a good starting point for further development of new antimicrobial compounds, where the next step would be tuning the potential between relatively nonspecific membrane depolarization effect and specific inhibition of proteosynthesis. | en |
dc.language.iso | en | |
dc.relation.url | http://www.future-science.com/doi/10.4155/fmc-2023-0189 | |
dc.rights | Creative Commons Uveďte původ 4.0 International | cs |
dc.rights | Creative Commons Attribution 4.0 International | en |
dc.title | N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation | en |
dcterms.accessRights | openAccess | |
dcterms.license | https://creativecommons.org/licenses/by/4.0/legalcode | |
dc.date.updated | 2024-04-03T09:40:41Z | |
dc.subject.keyword | antibacterial | en |
dc.subject.keyword | antimicrobial resistance | en |
dc.subject.keyword | antimycobacterial | en |
dc.subject.keyword | hit expansion | en |
dc.subject.keyword | macromolecular assay | en |
dc.subject.keyword | membrane depolarization | en |
dc.subject.keyword | minimum bactericidal concentration | en |
dc.subject.keyword | structure-activity relationship | en |
dc.subject.keyword | water solubility | en |
dc.relation.fundingReference | info:eu-repo/grantAgreement/FN/I-FN/I-FNHK | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/MZ0/NU/NU21-05-00482 | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/UK//SVV260666 | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/MSM//LX22NPO5103 | |
dc.relation.fundingReference | info:eu-repo/grantAgreement/UK/COOP/COOP | |
dc.date.embargoStartDate | 2024-04-03 | |
dc.type.obd | 73 | |
dc.type.version | info:eu-repo/semantics/publishedVersion | |
dc.identifier.doi | 10.4155/fmc-2023-0189 | |
dc.identifier.utWos | 001091474100001 | |
dc.identifier.eidScopus | 2-s2.0-85175742519 | |
dc.identifier.obd | 639764 | |
dc.identifier.pubmed | 37877255 | |
dc.subject.rivPrimary | 30000::30100::30104 | |
dcterms.isPartOf.name | Future Medicinal Chemistry | |
dcterms.isPartOf.issn | 1756-8919 | |
dcterms.isPartOf.journalYear | 2023 | |
dcterms.isPartOf.journalVolume | 15 | |
dcterms.isPartOf.journalIssue | 19 | |
uk.faculty.primaryId | 113 | |
uk.faculty.primaryName | Farmaceutická fakulta v Hradci Králové | cs |
uk.faculty.primaryName | Faculty of Pharmacy in Hradec Kralove | en |
uk.faculty.secondaryId | 51 | |
uk.faculty.secondaryName | Fakultní nemocnice Hradec Králové | cs |
uk.faculty.secondaryName | University Hospital Hradec Králové | en |
uk.department.primaryId | 373 | |
uk.department.primaryName | Katedra farmaceutické chemie a farmaceutické analýzy | cs |
uk.department.primaryName | Department of Pharmaceutical Chemistry and Pharmaceutical Analysis | en |
uk.department.secondaryId | 5000000039 | |
uk.department.secondaryId | 369 | |
uk.department.secondaryName | Ústav klinické mikrobiologie | cs |
uk.department.secondaryName | Department of Clinical Microbiology | en |
uk.department.secondaryName | Katedra biologických a lékařských věd | cs |
uk.department.secondaryName | Department of Biological and Medical Sciences | en |
dc.description.pageRange | 1791-1806 | |
dc.type.obdHierarchyCs | ČLÁNEK V ČASOPISU::článek v časopisu::původní článek | cs |
dc.type.obdHierarchyEn | JOURNAL ARTICLE::journal article::original article | en |
dc.type.obdHierarchyCode | 73::152::206 | en |
uk.displayTitle | N-Pyrazinylhydroxybenzamides as biologically active compounds: a hit-expansion study and antimicrobial evaluation | en |