Naslov (srp)

Sinteza, karakterizacija i biološka aktivnost nekih derivata kumarina i odgovarajućih Pd(II) kompleksa

Autor

Avdović, Edina H., 1979-

Doprinosi

Trifunović, Srećko, 1954-
Marković, Zoran, 1958-
Jevtić, Verica, 1976-
Vuković, Nenad, 1976-
Milenković, Dejan.
Radojević, Ivana, 1973-

Opis (srp)

Biljni ekstrakti koji sadrže derivate kumarina su se često koristili kao biljni lekovi. Iz tih razloga derivati kumarina su intenzivno proučavani i utvrđeno je da ova jedinjenja pokazuju značajne biološke osobine kao što su: antioksidativne, antikoagulacione, antimikrobne, antitumorske itd. S druge strane kompleksna jedinjenja sama ili u kombinaciji sa drugim jedinjenjima, već duži niz godina se koriste u medicini za lečenje brojnih bolesti. Ova jedinjenja imaju primenu u medicini kao antimikrobni agensi, za lečenjenje malignih bolesti, reumatskog artritisa itd. Zbog širokog spektra biološke aktivnosti kako derivata kumarina tako i kompleksnih jedinjenja u okviru ove doktorske disertacije sintetisano je devet novih derivata kumarina i osam odgovarajućih paladijuma(II) kompleksa i ispitivana je njihova in vitro biološka aktivnost. Derivati kumarina su korišćeni kao ligandi u sintezi paladijuma(II) kompleksa. Karakterizacija sintetisanih jedinjenja je izvršena pomoću: rendgenske stukturne analize, spektroskopskih (IR, 1H NMR i 13C NMR) i DFT metoda. Strukturna analiza je pokazala da sva jedinjenja formiraju šestočlani prsten preko intpamolekulske vodonične veze N−H···O, što omogućava da se molekuli javljaju u ketoenolnoj tautomernoj formi. Sva dobijena jedinjenja imaju E geometriju na egzocikličnoj dvostrukoj C3=C1' vezi. Rendgentska strukturna analiza i DFT metoda su potvrdile da su L1–L3 molekuli planarni, dok je za ostale molekule L4–L9 nađeno da kumarinski i anilinski delovi molekula nisu planarni. In vitro antimikrobna aktivnost sintetisanih liganada i odgovarajućih kompleksa paladijuma(II) testirana je mikrodilucionom i disk difuzionom metodom. Mikrodilucionom metodom određene su minimalne inhibitorne (MIC) i minimalne mikrobicidne koncentracije (MMC), dok disk difuzionom metodom je određena zona inhibicije (ZI) ispitivanih jedinjenja. Na osnovu rezultata antimikrobne analize utvrđeno je da jedinjenja L1–L6 i C1–C6 pokazuju slabu do umerene antimikrobnu aktivnost. S druge strane ligandi i kompleksi L7–L9 i C8 i C9 su pokazali veoma dobru antimikrobnu i antifungalnu aktivnost.

Opis (eng)

Herbal extracts, which contains coumarin derivatives, were often used as herbal remedies. For these reasons, the coumarin derivatives have been intensively studied and it has been found that these compounds indicate significant biological properties such as: antioxidant, anticoagulant, antimicrobial, antitumor, etc. On the other hand, complex compounds, alone or in combination with other compounds, have been used for many years in medicine for the treatment of many diseases. These compounds are used in medicine as antimicrobial agents, for the treatment of malignant diseases, rheumatoid arthritis, etc. Because of the wide range of biological activity, both coumarin derivatives and complex compounds, nine new coumarin derivatives and eight corresponding palladium(II) complexes were synthesized. For all of these compounds biological activity was tested in vitro. Coumarin derivatives were used as ligands in the synthesis of the palladium(II) complexes. The characterization of the synthesized compounds was determinate using X-ray structural analysis, spectroscopic (IR, 1H NMR and 13C NMR) and DFT methods. Structural analysis has shown that all compounds form a six-membered ring through the intramolecular hydrogen bond N−H···O, which allows the molecules to appear in the keto-enol tautomeric forms. For all compounds it was found E geometry on the exocyclic double C3 = C1' bond. X-ray structural analysis and DFT method confirmed that L1-L3 molecules are planar, while for other molecules L4-L9 it was found that coumarin and aniline moieties are not planar. In vitro antimicrobial activity of synthesized ligands and corresponding palladium(II) complexes was tested with microdilution and disc diffusion method. The microdilution method has determined the minimum inhibitory (MIC) and minimum microbicidal concentrations (MMC), while the disc diffusion method has determined the inhibition zone (ZI) of the investigated compounds. Based on the results of the antimicrobial analysis, it has been found that the compounds L1-L6 and C1-C6 have shown a low to moderate antimicrobial activity. On the other hand, ligands L7-L9 and complexes C8 and C9 have shown very good antimicrobial and antifungal activity

Jezik

srpski

Datum

2018

Licenca

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CC BY-NC-SA 2.0 AT

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