Current Topics in Medicinal Chemistry - Volume 25, Issue 27, 2025

Artemisinin and its semisynthetic derivatives are a group of bioactive chemicals obtained mostly from the extracts of Artemisia species that exert a significant amount of antimalarial activity while remaining relatively safe and tolerable. However, their effectiveness is not limited to malaria; it extends to a variety of human infectious diseases. Mostly the mode of action includes the generation of free radicals by breaking the endoperoxide link in its molecular structure, which facilitates the eradication of microbial species. Artemisinins are found to inhibit bacterial, viral, protozoal, helminth, and fungal infections. Their derivatives, like artemisone, a reversible inhibitor, target the viral replication cycle, and artesunate suppresses EBV infection by inhibiting the production of early EBV proteins. They were also found to be highly effective against Helicobacter pylori and Mycobacterium tuberculosis by generating peroxides in a time and concentration-dependent way. Other derivatives, such as artesunate, artemether, and arteether, have also shown antimicrobial activity that can be administered orally, rectally, intramuscularly, or intravenously. This review aims to provide a complete update on the antimicrobial applications of Artemisinin and its semi-synthetic derivatives, as well as derived dimers/trimers. The paper reflects a significant potential for the discovery of novel Artemisinin medications that can be used as supplementary treatments for various diseases. However, further translational and experimental research is required for optimization and the establishment of pharmacokinetic profiles. In addition, health authorities are also required to regulate the present Artemisinins and newly discovered derivatives to ensure their long-term effectiveness in the worldwide fight against antibiotic resistance.

Humans, animals, and plants possess small polypeptides known as antimicrobial peptides (AMPs), which are often positively charged. They are tiny, mostly basic peptides with a molecular weight of 2 to 9 kDa. They are a crucial part of plants' innate defense system, acting as effector molecules that provide a resistance barrier against pests and diseases. Plants have been found to contain antimicrobial peptides belonging to numerous families, including plant defensins, thionins, cyclotides, and others. An increase in pathogen resistance is achieved through the transgenic overexpression of the relevant genes, while pathogen mutants that are susceptible to peptides exhibit decreased pathogenicity. For many organisms, AMPs exhibit a wide range of antimicrobial activity against various pathogens and serve as a crucial line of defense. This review raises awareness about plant antimicrobial peptides (AMPs) as potential therapeutic agents in the pharmaceutical and medical fields, including treating fungal and bacterial diseases. It also provides a broad synopsis of the main AMP families found in plants, their mechanisms of action, and the factors that influence their antimicrobial activities.

The global rise of drug-resistant malaria parasites is becoming an increasing threat to public health, emphasizing the urgent need for the development of new therapeutic strategies. Artimisinin-based therapies, once the backbone of malaria treatment, are now at risk due to the resistance developed in parasites. The lack of a universally accessible malaria vaccine exacerbates this crisis, underscoring the need to explore new antimalarial drugs. A more comprehensive understanding of the parasites’s life cycle has revealed several promising targets, including enzymes, transport proteins, and essential metabolic pathways that the parasite relies on for its survival and proliferation. This review provides an in-depth analysis of the vulnerabilities displayed by Plasmodium and recent advances that highlight potential drug targets and candidate molecules.