Tetraoxanes: Synthetic and Medicinal Chemistry Perspective

Abstract

The discovery of artemisinin from Chinese medicinal plant, Artemisia annua in 1971, opened a new era in the malarial chemotherapy. This discovery was the beginning of exploring peroxides as potential replacements for the traditional antimalarial drugs such as chloroquine and mefloquine. The structurally simple class of peroxides that emerged from these studies was the 1,2,4,5-tetraoxanes. This study describes the current status of tetraoxane-based antimalarials that show significant promises because of their artemisinin-like activity. Literature from 1999 has been critically reviewed and an attempt has been made to discuss various synthetic methods and structure-activity relationship study among the series of tetraoxane-based compounds. © 2010 Wiley Periodicals, Inc. Med Res Rev.

Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani

“…Among these, trioxolanes and tetraoxanes have shown activity against different parasites, such as the protozoans Plasmodium spp. [10][11][12][13][14][15][16][17][18][19], Perkinsus spp. [20], and the parasitic flatworms Schistosoma spp [21].…”

Synthesis, antimalarial activity, heme binding and docking studies of 4-aminoquinoline–pyrimidine based molecular hybrids

“…1 According to 2013 WHO report, there were 207 million cases and 20 an estimated 627000 deaths due to malaria worldwide. 3 The disease is transmitted by female mosquitoes and is caused by five different species of the protozoan 25 Plasmodium parasite, namely, falciparum, vivax, malariae, ovale and knowlesi. 3 The disease is transmitted by female mosquitoes and is caused by five different species of the protozoan 25 Plasmodium parasite, namely, falciparum, vivax, malariae, ovale and knowlesi.…”

Synthesis of 4‐aminoquinoline‐1,2,3‐triazole and 4‐aminoquinoline‐1,2,3‐triazole‐1,3,5‐triazine Hybrids as Potential Antimalarial Agents

“…Triazole is another class of compounds that exhibit variety of biological activity such as antifungal (24), antibacterial (25,26), antitubercular (27), etc., and the compound can easily be prepared by click chemistry (28). Keeping these points in mind, and as a part of our ongoing program on development of novel antimalarials (29–33), we herein report synthesis and antimalarial activity evaluation of 4‐aminoquinoline‐triazole conjugates ( 3 ) and 4‐aminoquinoline‐triazine‐triazole conjugates ( 4 ) (Figure 1).…”