1,2,4,5‐Tetraoxane derivatives/hybrids as potent antimalarial endoperoxides: Chronological advancements, structure−activity relationship (SAR) studies and future perspectives

Malaria is a life‐threatening disease that affects tropical and subtropical regions worldwide. Various drugs were used to treat malaria, including artemisinin and derivatives, antibiotics (tetracycline, doxycycline), quinolines (chloroquine, amodiaquine), and folate antagonists (sulfadoxine and pyri...

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Published in:Medicinal research reviews 2024-09, Vol.44 (5), p.2266-2290
Main Authors: T. A., Abdul Rahaman, Rajendra, Thakar Neha, Suhas, Kshirsagar Prasad, Ippagunta, Sirish K., Chaudhary, Sandeep
Format: Article
Language:English
Subjects:
5‐tetraoxanes
antimalarial activity
Antiparasitic agents
Drug resistance
hybrid drugs
infectious disease
Malaria
multidrug‐resistant
peroxides
plasmodium
SAR
Steroids
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Summary:Malaria is a life‐threatening disease that affects tropical and subtropical regions worldwide. Various drugs were used to treat malaria, including artemisinin and derivatives, antibiotics (tetracycline, doxycycline), quinolines (chloroquine, amodiaquine), and folate antagonists (sulfadoxine and pyrimethamine). Since the malarial parasites developed drug resistance, there is a need to develop new chemical entities with high efficacy and low toxicity. In this context, 1,2,4,5‐tetraoxanes emerged as an essential scaffold and have shown promising antimalarial activity. To improve activity and overcome resistance to various antimalarial drugs; 1,2,4,5‐tetraoxanes were fused with various aryl/heteroaryl/alicyclic/spiro moieties (steroid‐based 1,2,4,5‐tetraoxanes, triazine‐based 1,2,4,5‐tetraoxanes, aminoquinoline‐based 1,2,4,5‐tetraoxanes, dispiro‐based 1,2,4,5‐tetraoxanes, piperidine‐based 1,2,4,5‐tetraoxanes and diaryl‐based 1,2,4,5‐tetraoxanes). The present review aims to focus on covering the relevant literature published during the past 30 years (1992–2022). We summarize the most significant in vitro, in vivo results and structure–activity relationship studies of 1,2,4,5‐tetraoxane‐based hybrids as antimalarial agents. The structural evolution of different hybrids can provide the framework for the future development of 1,2,4,5‐tetraoxane‐based hybrids to treat malaria.
ISSN:0198-6325
1098-1128
1098-1128
DOI:10.1002/med.22040