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Synthesis, Characterization and Complex Evaluation of Antibacterial Activity and Cytotoxicity of New Arylmethylidene Ketones and Pyrimidines with Camphane Skeletons

2022-05-03Journal article Restricted access
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dc.contributor.authorSlavchev, Ivaylo M.
dc.contributor.authorMitrev, Yavor
dc.contributor.authorShivachev, Boris
dc.contributor.authorValcheva, Violeta
dc.contributor.authorDogonadze, Marine
dc.contributor.authorSolovieva, Natalia
dc.contributor.authorVyazovaya, Anna
dc.contributor.authorMokrousov, Igor
dc.contributor.authorLink, Wolfgang
dc.contributor.authorJiménez, Lucía
dc.contributor.authorCautain, Bastien
dc.contributor.authorMackenzie, Thomas A.
dc.contributor.authorPortugal, Isabel
dc.contributor.authorLopes, Francisca
dc.contributor.authorCapela, Rita
dc.contributor.authorPerdigão, João
dc.contributor.authorDobrikov, Georgi M.
dc.date.accessioned2023-08-18T11:27:17Z
dc.date.available2023-08-18T11:27:17Z
dc.date.issued2022-05-03
dc.date.updated2023-01-04T15:28:02Z
dc.description.abstractThe synthesis of 20 arylidenecamphors and 15 pyrimidines with camphane skeleton is described in the current report. A modified method for preparation of sterically hindered 2-aminopyrimidines in two steps was demonstrated. The evaluation of their in vitro activity against Mycobacterium tuberculosis H37Rv showed different MIC values (up to 0.91 μM for ketone 39). Compound 35 demonstrated moderate (8.23 μM), but sustainable activity toward a collection of drug-resistant M. tuberculosis strains. Many of the compounds (especially among 2-aminopyridines 42–56) exhibited good to excellent activity against different strains of pathogenic bacteria and fungi (MIC up to 0.60 μM for compound 50), compared with reference antibiotics. Many of the newly designed compounds possess also in vitro cytotoxicity.pt_PT
dc.description.sponsorshipAuthors would like to thank COST Action STRATAGEM, CA17104, “New diagnostic and therapeutic tools against multidrug resistant tumors” supported by COST (European Cooperation in Science and Technology) (www.cost.eu, accessed in July 2021). This study was supported by: Bulgarian National Science Fund - project KP-06-H39/7 and Spanish Ministry of Science, Innovation and Universities - Grant RTI2018-094629-B I00. MEDINA’s authors disclosed the receipt of financial support from Fundación MEDINA, a public-private partnership of Merck Sharp and Dohme de España S.A./Universidad de Granada/Junta de Andalucíapt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationSlavchev IM, Mitrev Y, Shivachev B, Valcheva V, Dogonadze M, Solovieva N, et al. Synthesis, characterization and complex evaluation of antibacterial activity and cytotoxicity of new arylmethylidene ketones and pyrimidines with camphane skeletons. ChemistrySelect [Internet]. 6 de maio de 2022;7(17). Disponível em: https://chemistry-europe.onlinelibrary.wiley.com/doi/epdf/10.1002/slct.202201339pt_PT
dc.identifier.doi10.1002/slct.202201339pt_PT
dc.identifier.issn2365-6549
dc.identifier.slugcv-prod-3107708
dc.identifier.urihttp://hdl.handle.net/10451/58922
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherWiley-VCHpt_PT
dc.relation.publisherversionhttps://chemistry-europe.onlinelibrary.wiley.com/doi/epdf/10.1002/slct.202201339pt_PT
dc.subjectantibioticspt_PT
dc.subjectcamphorpt_PT
dc.subjectcytotoxicitypt_PT
dc.subjectdrug-discoverypt_PT
dc.subjectheterocyclespt_PT
dc.subjecttuberculosipt_PT
dc.titleSynthesis, Characterization and Complex Evaluation of Antibacterial Activity and Cytotoxicity of New Arylmethylidene Ketones and Pyrimidines with Camphane Skeletonspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue17pt_PT
oaire.citation.startPagee202201339pt_PT
oaire.citation.titleChemistrySelectpt_PT
oaire.citation.volume7pt_PT
person.familyNamePortugal
person.familyNameLopes
person.familyNameCapela
person.familyNameLucas Mota Perdigão
person.givenNameIsabel
person.givenNameFrancisca
person.givenNameRita
person.givenNameJoão Ruben
person.identifier.ciencia-idE310-5746-C205
person.identifier.ciencia-id3911-17F9-540E
person.identifier.ciencia-id801D-647D-1F16
person.identifier.ciencia-id991C-F26A-9843
person.identifier.orcid0000-0002-7843-0006
person.identifier.orcid0000-0002-5350-147X
person.identifier.orcid0000-0001-9637-3714
person.identifier.orcid0000-0002-0339-1305
person.identifier.ridA-6002-2016
person.identifier.scopus-author-id6602816287
person.identifier.scopus-author-id24723211800
rcaap.cv.cienciaid991C-F26A-9843 | João Ruben Lucas Mota Perdigão
rcaap.rightsclosedAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication4484da69-843c-4a20-af02-b3c111f84324
relation.isAuthorOfPublication914c2246-322f-4b77-85e8-d1e0c22e21d6
relation.isAuthorOfPublication5a363f6b-fddd-4922-9b78-b145a1d04903
relation.isAuthorOfPublication26de40fc-fc1d-4ff9-a242-3bb398e3ac1e
relation.isAuthorOfPublication.latestForDiscovery4484da69-843c-4a20-af02-b3c111f84324

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