300823-47-6Relevant articles and documents
Structure-activity relationship and molecular modelling studies of quinazolinedione derivatives MMV665916 as potential antimalarial agent
Albrecht, Sébastien,Florent, Isabelle,Mouray, Elisabeth,Mourot, Laura,Schmitt, Marjorie,Spichty, Martin
, (2021/11/22)
A series of new quinazolinedione derivatives have been readily synthesized and evaluated for their in vitro antiplasmodial growth inhibition activity. Most of the compounds inhibited P. falciparum FcB1 strain in the low to medium micromolar concentration. The 2-ethoxy 8ag’, 2-trifluoromethoxy 8ai’ and 4-fluoro-2-methoxy 8ak’ showed the best inhibitory activity with EC50 values around 5 μM and were non-toxic to the primary human fibroblast cell line AB943. However, these compounds were less potent than the original hit MMV665916, which showed remarkable growth inhibition with EC50 value of 0.4 μM and presented the highest selectivity index (SI > 250). In addition, a novel approach for determining the docking poses of these quinazolinedione derivatives with their potential protein target, the P. falciparum farnesyltransferase PfFT, was investigated.
Carcarinic acid-1, 2, 3- based triazole compound as well as preparation method and application thereof (by machine translation)
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Paragraph 0145-0147, (2019/12/25)
The method comprises the following steps: firstly 1, 2, 3 - oxidizing and opening the carbon- carbon double bond of the, carcarinic acid into methylene to, obtain carcarinic acid (not shown, in the technical field of, organic 3 - synthesis), Wolf - Kishner - 1, 2, 3 - 1, 2, 3 - 1, 2, 3 - 3 . (by machine translation)
Synthesis, Characterization, and Antimicrobial Activity of a Series of 2-(5-Phenyl-1,3,4-oxadiazol-2-yl)-N-[(1-aryl-1H-1,2,3-triazol-4-yl)methyl]anilines Using Click Chemistry
Venkatagiri,Krishna,Thirupathi,Bhavani,Reddy
, p. 1488 - 1494 (2018/09/10)
series of new triazolyl derived 1,3,4-oxadiazoles 7a–7l is synthesized with high yields by coppercatalyzed alkyne–azide cycloaddition reaction between a variety of substituted aryl/alkyl azides and 2-(5-phenyl-1,3,4-oxadiazol-2-yl)aniline. Structures of intermediates and the final compounds are confirmed by FTIR, 1H and 13C NMR, and Mass spectra. The synthesized compounds demonstrate moderate antibacterial activity and potent antifungal activity against the tested strains.