On peroxide antimalarials
O peroksidnim antimalaricima
2007
Autori
Opsenica, IgorOpsenica, Dejan M.
Jadranin, Milka
Smith, Kirsten S.
Milhous, Wilbur K.
Stratakis, Manolis
Šolaja, Bogdan A.
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized.
U ovom radu prikazana je sinteza nekoliko dicikiloheksilidenskih tetraoksana u cilju sagledavanja odnosa struktura-aktivnost ove vrste antimalarika. Jedinjenja 2-5 dobijena kao (cis,trans)-smese pokazala su izraženu antimalarijsku aktivnost prema D6, W2 i TM91C235 (Thailand) sojevima P. falciparum. Ona imaju bolju ili sličnu aktivnost od odgovarajućih desmetil cikloheksilidenskih derivata. Sintetisana su i dva endoperoksida himerne strukture znatno izraženije aktivnosti od prirodnog proizvoda askaridola. .
Ključne reči:
mixed tetraoxanes / endoperoxides / endoperoxides / malaria / malaria / P. falciparum / P. falciparumIzvor:
Journal of the Serbian Chemical Society, 2007, 72, 12, 1181-1190Izdavač:
- Serbian Chemical Soc, Belgrade
Finansiranje / projekti:
- Peroksidni antimalarici i njihove himere sa hinolinima: sinteza i biološka aktivnost (RS-MESTD-MPN2006-2010-142022)
DOI: 10.2298/JSC0712181O
ISSN: 0352-5139
WoS: 000252412100003
Scopus: 2-s2.0-36949031727
Kolekcije
Institucija/grupa
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Opsenica, Igor AU - Opsenica, Dejan M. AU - Jadranin, Milka AU - Smith, Kirsten S. AU - Milhous, Wilbur K. AU - Stratakis, Manolis AU - Šolaja, Bogdan A. PY - 2007 UR - https://cherry.chem.bg.ac.rs/handle/123456789/901 AB - Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized. AB - U ovom radu prikazana je sinteza nekoliko dicikiloheksilidenskih tetraoksana u cilju sagledavanja odnosa struktura-aktivnost ove vrste antimalarika. Jedinjenja 2-5 dobijena kao (cis,trans)-smese pokazala su izraženu antimalarijsku aktivnost prema D6, W2 i TM91C235 (Thailand) sojevima P. falciparum. Ona imaju bolju ili sličnu aktivnost od odgovarajućih desmetil cikloheksilidenskih derivata. Sintetisana su i dva endoperoksida himerne strukture znatno izraženije aktivnosti od prirodnog proizvoda askaridola. . PB - Serbian Chemical Soc, Belgrade T2 - Journal of the Serbian Chemical Society T1 - On peroxide antimalarials T1 - O peroksidnim antimalaricima VL - 72 IS - 12 SP - 1181 EP - 1190 DO - 10.2298/JSC0712181O ER -
@article{ author = "Opsenica, Igor and Opsenica, Dejan M. and Jadranin, Milka and Smith, Kirsten S. and Milhous, Wilbur K. and Stratakis, Manolis and Šolaja, Bogdan A.", year = "2007", abstract = "Several dicyclohexylidene tetraoxanes were prepared in order to gain a further insight into structure-activity relationship of this kind of antimalarials. The tetraoxanes 2-5, obtained as a cis/trans mixture, showed pronounced antimalarial activity against Plasmodium falciparum chloroquine susceptible D6, chloroquine resistant W2 and multidrug-resistant TM91C235 (Thailand) strains. They have better than or similar activity to the corresponding desmethyl dicyclohexylidene derivatives. Two chimeric endoperoxides with superior antimalarial activity to the natural product ascaridole were also synthesized., U ovom radu prikazana je sinteza nekoliko dicikiloheksilidenskih tetraoksana u cilju sagledavanja odnosa struktura-aktivnost ove vrste antimalarika. Jedinjenja 2-5 dobijena kao (cis,trans)-smese pokazala su izraženu antimalarijsku aktivnost prema D6, W2 i TM91C235 (Thailand) sojevima P. falciparum. Ona imaju bolju ili sličnu aktivnost od odgovarajućih desmetil cikloheksilidenskih derivata. Sintetisana su i dva endoperoksida himerne strukture znatno izraženije aktivnosti od prirodnog proizvoda askaridola. .", publisher = "Serbian Chemical Soc, Belgrade", journal = "Journal of the Serbian Chemical Society", title = "On peroxide antimalarials, O peroksidnim antimalaricima", volume = "72", number = "12", pages = "1181-1190", doi = "10.2298/JSC0712181O" }
Opsenica, I., Opsenica, D. M., Jadranin, M., Smith, K. S., Milhous, W. K., Stratakis, M.,& Šolaja, B. A.. (2007). On peroxide antimalarials. in Journal of the Serbian Chemical Society Serbian Chemical Soc, Belgrade., 72(12), 1181-1190. https://doi.org/10.2298/JSC0712181O
Opsenica I, Opsenica DM, Jadranin M, Smith KS, Milhous WK, Stratakis M, Šolaja BA. On peroxide antimalarials. in Journal of the Serbian Chemical Society. 2007;72(12):1181-1190. doi:10.2298/JSC0712181O .
Opsenica, Igor, Opsenica, Dejan M., Jadranin, Milka, Smith, Kirsten S., Milhous, Wilbur K., Stratakis, Manolis, Šolaja, Bogdan A., "On peroxide antimalarials" in Journal of the Serbian Chemical Society, 72, no. 12 (2007):1181-1190, https://doi.org/10.2298/JSC0712181O . .