Discovery of Antimalarial Drug Artemisinin and Beyond

Peroxides with Anthelmintic, Antiprotozoal, Fungicidal and Antiviral Bioactivity: Properties, Synthesis and Reactions

“…Antimalarial properties of peroxides are currently intensively studied. Artemisinin (Qinghaosu) ( 1 ), a natural peroxide possessing high antimalarial activity, was isolated in 1971 from leaves of annual wormwood ( Artemisia annua ) in the context of the scientific program “Project 523”, initiated by Chinese government in 1967 [ 18 , 19 , 20 ]. The Nobel Prize in Physiology or Medicine 2015 was awarded to Chinese pharmaceutical chemist Tu Youyou “for her discoveries concerning a novel therapy against Malaria” [ 21 , 22 , 23 ].…”

Peroxy natural products

“…Its antimalarial activity, structural modification, structure-activity relationships, mode of actions, and use in therapy have been well reviewed. [237][238][239][240] 3.3 Diterpenes: A dolabellane diterpene derivative 401 with the naturally rare peroxy function was identified as a component of the aerial parts of Cleome droserifolia, 241 and additional related peroxide 402 was found from Aglaia odorata. 242 Jatropha integerrima provided a rhamnofolane endoperoxide 2-epicaniojane 403, whose structure was confirmed by X-ray diffraction analysis.…”

Synthesis and biological investigation of (+)-3-hydroxymethylartemisinin

“…In the past, several semi-synthetic artemisinin derivatives were prepared for experimental therapy of pathologies like the ones mentioned before [12–13]. However, the variety of these derivatives is limited as all of them are produced modifying the artemisinin skeleton at the same positions due to intrinsic synthetic challenges.…”