Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives - Aix-Marseille Université Access content directly
Journal Articles Journal of the Iranian Chemical Society Year : 2018

Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives

Abstract

This paper describes the synthesis of some new beta-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 mu M 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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hal-02143574 , version 1 (29-05-2019)

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Aliasghar Jarrahpour, Malihe Aye, Javad Ameri Rad, Saeed Yousefinejad, Veronique Sinou, et al.. Design, synthesis, activity evaluation and QSAR studies of novel antimalarial 1,2,3-triazolo-beta-lactam derivatives. Journal of the Iranian Chemical Society, 2018, 15 (6), pp.1311-1326. ⟨10.1007/s13738-018-1330-2⟩. ⟨hal-02143574⟩
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