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https://doi.org/10.2478/v10007-010-0004-0

Sinteza i biološko djelovanje novih 1-benzil i 1-benzoil 3-heterocikličkih derivata indola

ESLAM REDA EL-SAWY ; Chemistry Department of Natural Compounds, National Research Centre, Cairo, Egypt
FATMA A. BASSYOUNI ; Chemistry Department of Natural and Microbial Products, National Research Centre, Cairo, Egypt
SHERIFA H. ABU-BAKR ; Chemistry Department of Natural and Microbial Products, National Research Centre, Cairo, Egypt
HANAA M. RADY ; Chemistry Department of Natural Compounds, National Research Centre, Cairo, Egypt
MOHAMED M. ABDLLA ; Univeterinary Research Unit, Pharmaceutical Company, Cairo, Egypt

Puni tekst: engleski, pdf (108 KB) str. 55-71 preuzimanja: 989* citiraj
APA 6th Edition
EL-SAWY, E.R., BASSYOUNI, F.A., ABU-BAKR, S.H., RADY, H.M. i ABDLLA, M.M. (2010). Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives. Acta Pharmaceutica, 60 (1), 55-71. https://doi.org/10.2478/v10007-010-0004-0
MLA 8th Edition
EL-SAWY, ESLAM REDA, et al. "Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives." Acta Pharmaceutica, vol. 60, br. 1, 2010, str. 55-71. https://doi.org/10.2478/v10007-010-0004-0. Citirano 26.06.2019.
Chicago 17th Edition
EL-SAWY, ESLAM REDA, FATMA A. BASSYOUNI, SHERIFA H. ABU-BAKR, HANAA M. RADY i MOHAMED M. ABDLLA. "Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives." Acta Pharmaceutica 60, br. 1 (2010): 55-71. https://doi.org/10.2478/v10007-010-0004-0
Harvard
EL-SAWY, E.R., et al. (2010). 'Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives', Acta Pharmaceutica, 60(1), str. 55-71. doi: https://doi.org/10.2478/v10007-010-0004-0
Vancouver
EL-SAWY ER, BASSYOUNI FA, ABU-BAKR SH, RADY HM, ABDLLA MM. Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives. Acta Pharm. [Internet]. 2010 [pristupljeno 26.06.2019.];60(1):55-71. doi: https://doi.org/10.2478/v10007-010-0004-0
IEEE
E.R. EL-SAWY, F.A. BASSYOUNI, S.H. ABU-BAKR, H.M. RADY i M.M. ABDLLA, "Synthesis and biological activity of some new 1-benzyl and 1-benzoyl 3-heterocyclic indole derivatives", Acta Pharmaceutica, vol.60, br. 1, str. 55-71, 2010. [Online]. doi: https://doi.org/10.2478/v10007-010-0004-0

Sažetak
U radu je opisana sinteza, antimikrobno i antitumorsko djelovanje heterocikličkih derivata indola. Polazeći iz 1-benzil- i 1-benzoil-3-bromacetil indola (2a i 2b) sintetizirani su novi heterociklički spojevi 2-tioksoimidazolidini (4a,b), imidazolidin-2,4-dioni (5a,b), pirano(2,3-d)imidazoli (8a,b i 9a,b), 2-supstituirani kinoksalini (11a,b–17a,b) i triazolo(4,3-a)kinoksalini (18a,b i 19a,b). Sintetizirani spojevi testirani su na antimikrobno i antitumorsko djelovanje. Ispitivanje antimikrobnog djelovanja provedeno je s koncentracijama otopina 0,88, 0,44 i 0,22 g mm2 i uspoređeno s referentnim lijekovima cefotaksimom i piperacilinom. Rezultati pokazuju da su 3-(1-supstituirani indol-3-il)kinoksalin-2(1H)oni (11a,b) i 2-(4-metil piperazin-1-il)-3-(1-supstituirani indol-3-il) kinoksalini (15a,b) najaktivniji spojevi na sojeve P. aeruginosa, B. cereus i S. aureus, dok su 2-klor-3-(1-supstituirani indol-3-il)kinoksalini (12a,b) najaktivniji na C. albicans (usporedba s nistatinom). Osim toga, 2-klor-3-(1-benzil indol-3-il) kinoksalin (12a) pokazuje veliku učinkovitost na tumore ovarija miševa (supresija rasta tumora 100  0,3 %).

Ključne riječi
2-klor-3-(1-benzil)kinoksalini; 2-klor-3-(1-benzoilindol-3-il)kinoksalini; antimikrobno djelovanje; antitumorsko djelovanje

Hrčak ID: 48278

URI
https://hrcak.srce.hr/48278

[engleski]

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