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design, synthesis, activity evaluation and qsar studies of novel antimalarial 1,2,3-triazolo-β-lactam derivatives
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نویسنده
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jarrahpour aliasghar ,aye malihe ,rad javad ameri ,yousefinejad saeed ,sinou véronique ,latour christine ,brunel jean michel ,turos edward
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منبع
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journal of the iranian chemical society - 2018 - دوره : 15 - شماره : 6 - صفحه:1311 -1326
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چکیده
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This paper describes the synthesis of some new β-lactam derivatives containing the 1,2,3-triazole moiety. all the compounds were evaluated for their in vitro antimicrobial and antimalarial activities. moderate to excellent antimalarial activities were encountered. the results showed that compounds 5a, 5c, 5f, 5i exhibited the most potent antimalarial activity with ic50 values of 0.85, < 0.97, < 0.97, 1.81 µm against chloroquine-resistant p. falciparum k1 strain. a qsar study highlights the structure–activity relationships that correlate the observed antimalarial activities with changes in the compounds’ structural features.
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کلیدواژه
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imine ,3-triazole ,staudinger reaction ,antimalarial activities ,chloroquine ,qsar
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آدرس
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shiraz university, college of sciences, department of chemistry, iran, shiraz university, college of sciences, department of chemistry, iran, shiraz university, college of sciences, department of chemistry, iran, shiraz university of medical sciences, research center for health sciences, institute of health, school of health, department of occupational health engineering, iran, aix-marseille université, faculté de pharmacie, france, aix-marseille université, faculté de pharmacie, france, aix-marseille université, centre de recherche en cancerologie de marseille (crcm), institut paoli calmettes, faculté de pharmacie, france, university of south florida, center for molecular diversity in drug design, department of chemistry, usa
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Authors
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