Chemical insights into artemisinin's biological mechanism of action have allowed rational design of some new trioxane and endoperoxide antimalarial drug candidates that are efficacious and safe. This review summarizes recent achievements in this area of peroxide drug development for malaria chemotherapy.
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http://dx.doi.org/10.2174/1389557023405620 | DOI Listing |
J Heterocycl Chem
September 2024
Biochemistry, Chemistry and Physics Department, Georgia Southern University, PO Box 8064, Statesboro, GA 30460.
9-Aminoacridine structures hold much potential for accessing small molecule therapeutics. This core is present in a range of pharmaceuticals for the treatment of ailments such as malaria, inflammation, viral and bacterial infections, and cancer. For the latter, there remains a need to develop and/or improve chemotherapeutics to counteract issues of uptake, drug resistance, and selectivity for cancer cells over healthy cells.
View Article and Find Full Text PDFJACS Au
October 2024
Department of Parasitology, Institute of Biomedical Sciences, University of São Paulo, São Paulo, SP 05508-000, Brazil.
Malaria control and elimination efforts would benefit from the identification and validation of new malaria chemotherapeutics. Recently, a transgenic line was used to perform a series of high-throughput in vitro screens for new antimalarials acting against the parasite sexual stages. The screens identified pyrimidine azepine chemotypes with potent activity.
View Article and Find Full Text PDFCurr Pharm Des
September 2024
University Institute of Pharma Sciences, Chandigarh University, Mohali, Punjab, India.
More than two hundred million people around the world are infected with malaria, a blood-borne disease that poses a significant risk to human life. Single medications, such as lumefantrine, primaquine, and chloroquine, as well as combinations of these medications with artemisinin or its derivatives, are currently being used as therapies. In addition, due to rising antimalarial drug resistance, other therapeutic options are needed immediately.
View Article and Find Full Text PDFNat Commun
August 2024
School of Biological Sciences, Nanyang Technological University (NTU), Singapore, 637551, Singapore.
Recrudescent infections with the human malaria parasite, Plasmodium falciparum, presented traditionally the major setback of artemisinin-based monotherapies. Although the introduction of artemisinin combination therapies (ACT) largely solved the problem, the ability of artemisinin to induce dormant parasites still poses an obstacle for current as well as future malaria chemotherapeutics. Here, we use a laboratory model for induction of dormant P.
View Article and Find Full Text PDFCurr Med Chem
August 2024
Medicinal Chemistry Laboratory, Department of Biosciences, Jamia Millia Islamia, New Delhi, India.
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