Abstract: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 concentrationdependent
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.