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

Aliasghar Jarrahpour Malihe Aye Javad Ameri Rad Saeed Yousefinejad 1 Veronique Sinou 2 Christine Latour 2 Jean Michel Brunel 3, 4 Edward Turos
1 Shiraz University - Shiraz University
2 IP-TPT - Infections Parasitaires : Transmission, Physiopathologie et Thérapeutiques
3 MCT - Membranes et cibles thérapeutiques
4 CRCM - Centre de Recherche en Cancérologie de Marseille
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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https://hal-amu.archives-ouvertes.fr/hal-02143574
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Submitted on : Wednesday, May 29, 2019 - 2:48:32 PM
Last modification on : Wednesday, August 19, 2020 - 12:08:17 PM

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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- Iranian Chemical Society, Iranian Chemical Society, 2018, 15 (6), pp.1311-1326. ⟨10.1007/s13738-018-1330-2⟩. ⟨hal-02143574⟩

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