Structure-activity relationship of anti-malarial spongean peroxides having a 3-methoxy-1,2-dioxane structure

Bioorganic & Medicinal Chemistry
Motoyuki KawanishiMotomasa Kobayashi

Abstract

In order to study the structure-activity relationship of anti-malarial spongean peroxides, several analogues concerning with the 6-methoxyacetyl moiety and the 3-pentyl residue in methyl 2-(3-methoxy-3-pentyl-1,2-dioxan-6-yl)acetate were synthesized and evaluated for anti-malarial activity. The tert-butyl ester analogue 14 showed stability in mouse serum and a high selectivity index against the malaria parasite, Plasmodium falciparum, and the citronellyl analogue 31 exhibited the strongest in vitro anti-malarial activity among them, and the imidazole analogue 25 showed desirable in vivo anti-malarial activity against P. berghei infected mice.

References

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Citations

Jun 6, 2008·Journal of the American Chemical Society·Xiaojie LuLi Deng
Oct 23, 2015·Organic Letters·Christophe DaeppenKarl Gademann
May 16, 2006·Medicinal Research Reviews·Suryanaryana VangapanduRahul Jain
Aug 27, 2009·Organic & Biomolecular Chemistry·Xin FengYing-Chun Chen
Jul 28, 2010·Angewandte Chemie·Wenhua ZhengJon C Antilla
Feb 6, 2010·Organic & Biomolecular Chemistry·Orazio Taglialatela-ScafatiCaterina Fattorusso
Jan 24, 2014·Beilstein Journal of Organic Chemistry·Alexander O Terent'evValery M Dembitsky
Mar 5, 2010·The Journal of Organic Chemistry·Sandra GemmaStefania Butini
May 1, 2009·The Journal of Organic Chemistry·Reiko UeokaNobuhiro Fusetani
Jul 19, 2011·Organic Letters·Hong-Dong HaoYikang Wu

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