Design of pharmacophoric group containing 1,4-dihydropyridine derivatives and determination of spectrum of pharmacological activities

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dc.contributor.advisorMuceniece, Ruta
dc.contributor.advisorPlotniece, Aiva
dc.contributor.authorRuciņš, Mārtiņš
dc.contributor.otherLatvijas Universitāte. Medicīnas fakultāte
dc.date.accessioned2017-03-24T02:01:10Z
dc.date.available2017-03-24T02:01:10Z
dc.date.issued2017
dc.description.abstractVairākkārtīgi ir uzsvērts, ka 1,4-dihidropiridīna cikls ir viens no farmakoloģiski priviliģētām struktūrām, kas iedarbojas uz jonu kanāliem un dažādiem receptoriem, un kuru modificējot, sintezējot tās struktūras analogus, variējot aizvietotājus molekulā, būtu iespējams iegūt dažādus farmakoloģiski aktīvus savienojumus. Pētījumā ir sintezēti jauni, mērķtiecīgi dizainēti, farmakoforas grupas saturoši 1,4-dihidropiridīna atvasinājumi, sistemātiski mainot farmakoforās grupas (piridīniju un/vai propargil) un to atrašanās vietu molekulā. Izvērtēts sintezēto savienojumu farmakoloģiskās darbības spektrs (aktivitāte uz kalcija kanāliem, antiradikālā aktivitāte un reducējošā kapacitāte), veidots struktūras-aktivitātes likumsakarību modelis, meklējot jaunus farmakoloģiski aktīvus savienojumus. Pētīta pašasociējošos 1,4-dihidropiridīna atvasinājumu nanodaļiņu veidošanās un to stabilitāte.
dc.description.abstract1,4-Dihydropyridine cycle is one of pharmacologically privileged structures acting on ion channels and various receptors. Modification of the 1,4-dihydropyridine cycle by synthesis of structural analogues, varying substituents in the molecule provides the approach to give a variety of pharmacologically active compounds. In this thesis were synthesized new, targeted designed, pharmacophoric group containing 1,4-dihydropyridine derivatives by purposeful changing of pharmacophoric groups (pyridinium and/or propargyl) and their location in the molecule. Analyzed a spectrum of pharmacological properties of synthesized compounds (calcium channel activity, antiradical activity and reducing capacity), created the structure-activity relationship model for search of new pharmacologically active compounds. Studied properties of nanoparticle formation and stability of synthesized self-assembling 1,4-dihydropyridine derivatives.
dc.description.sponsorshipThis work has been supported by the European Social Fund within the project „Support for Doctoral Studies at University of Latvia” and by the young researcher grant of the Latvian Institute of Organic Synthesis (IG-2016-10)
dc.identifier.other57063
dc.identifier.urihttps://dspace.lu.lv/dspace/handle/7/34911
dc.language.isoeng
dc.publisherLatvijas Universitāte
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectFarmācija
dc.subjectFarmaceitiskā ķīmija
dc.subjectPharmacy
dc.subjectPharmaceutical chemistry
dc.subject1,4-dihydropyridines
dc.subjectpyridinium
dc.subjectpropargyl group
dc.subjectPharmacophore
dc.subjectcalcium channel activity
dc.subjectantiradical activity
dc.subjectReducing capacity
dc.subjectnanoparticles
dc.titleDesign of pharmacophoric group containing 1,4-dihydropyridine derivatives and determination of spectrum of pharmacological activities
dc.title.alternativeFarmakoforas grupassaturošu 1,4-dihidropiridīna atvasinājumu dizains un to farmakoloģiskās darbības spektra noteikšana
dc.typeinfo:eu-repo/semantics/doctoralThesis
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