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2021, vol. 10, br. 2, str. 14-23
Sinteza, karakterizacija i procena antioksidativne i antimikrobne aktivnosti tri nova n-heteroaromatična hidrazonil-tiazola
aUniverzitet u Beogradu, Hemijski fakultet
bUniverzitet u Beogradu, Institut za hemiju, tehnologiju i metalurgiju - IHTM
cUniverzitet u Beogradu, Poljoprivredni fakultet

e-adresanenadf@agrif.bg.ac.rs
Projekat:
Ministarstvo prosvete, nauke i tehnološkog razvoja Republike Srbije (institucija: Inovacioni centar Hemijskog fakulteta u Beogradu doo) (MPNTR - 451-03-68/2020-14/200288)
Ministarstvo prosvete, nauke i tehnološkog razvoja Republike Srbije (institucija: Univerzitet u Beogradu, Hemijski fakultet) (MPNTR - 451-03-68/2020-14/200168)
Ministarstvo prosvete, nauke i tehnološkog razvoja Republike Srbije (institucija: Univerzitet u Beogradu, Institut za hemiju, tehnologiju i metalurgiju - IHTM) (MPNTR - 451-03-68/2020-14/200026)

Sažetak
(Tiazolil-2-il)-hidrazoni (TH) su grupa organskih jedinjenja koja sadrže i hidrazon i 1,3-tiazol farmakofore koje su prisutne u mnogim odobrenim lekovima. Poslednjih godina se u velikoj meri istražuju zbog jakih antikancerogenih, antibakterijskih, antifungalnih, antituberkuloznih, antiinflamatornih i antiparazitskih aktivnosti. U ovoj studiji, sintetisan je jedan novi TH na bazi piridina i dva na bazi hinolina, koji su okarakterisani elementalnom analizom, infracrvenom spektroskopijom sa Furijeovom transformacijom (FTIR) i spektroskopijom nuklearne magnetne rezonancije (NMR). Antimikrobna aktivnost jedinjenja je testirana na pet Gram-pozitivnih i pet Gram-negativnih bakterijskih sojeva, kao i na tri soja gljivica. Šest antioksidativnih testova je korišćeno za određivanje antioksidativnog kapaciteta sintetisanih jedinjenja. Rezultati su pokazali da su TH na bazi hinolina aktivniji prema testiranim Gram-negativnim sojevima bakterija i prema gljivicama, nego jedinjenja na bazi piridina. Sva jedinjenja su pokazala odlično antioksidativno dejstvo, uporedivo ili veće od korišćenih standarda (vitamin C i troloks). Parametri apsorpcije, distribucije, metabolizma, izlučivanja i toksičnosti (ADME) izračunati su in-silico. Rezultati ukazuju na dobre farmakokinetičke profile ispitivanih jedinjenja, posebno jedinjenja na bazi 2-hinolinkarboksaldehida koje ima potencijal da bude kandidat za osnovno jedinjenje (engl. lead compound).
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O članku

jezik rada: engleski
vrsta rada: izvorni naučni članak
DOI: 10.5937/savteh2102014K
primljen: 24.09.2021.
prihvaćen: 30.09.2021.
objavljen u SCIndeksu: 10.12.2021.

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