Validating targets antiparasitic chemotherapy

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N-Glycosylated DHA-piperazine derivatives were obtained according to the Kotchetkov reaction by heating the DHA-piperazine with the sugar in a polar solvent.

validating targets antiparasitic chemotherapy-3validating targets antiparasitic chemotherapy-35validating targets antiparasitic chemotherapy-58

The present Special Issue, meant as a joint publication platform for Medicinal and Natural Product Chemists and researchers from related fields as members of the COST Action CM1307 Working Groups 2 and 3, dedicated to Medicinal Chemistry and Natural products, respectively, focuses on chemical entities that show a promising potential to act against the pathogens responsible for the diseases under study.

All aspects related to the discovery and further development of synthetic and natural products against such endoparasitoses will be covered by the issue.

Needless to say that these diseases, for a long time restricted mostly to poor, underdeveloped parts of the world, are now—in these times of climate change and unhindered migration—spreading to all parts of the planet and thus may shortly become a truly global problem.

It is a great pleasure and an important political sign that the European Union has decided to dedicate one of its actions for European Cooperation in Science and Technology, COST action CM1307, to “Targeted chemotherapy towards diseases caused by endoparasites” and allows researchers from all relevant fields to participate in this quest of global importance!

The D-galactose, L-rhamnose and D-xylose derivatives displayed IC of 0.26 µM, and a SI of 88 with the same cell lines.

Overall, the N-glycosylated DHA-piperazine derivatives display antimalarial activities that are greatly superior to O-glycosides previously obtained from DHA.NTDs comprise, besides some infections with bacterial (e.g., Leprosy, Trachoma) and viral (Dengue fever) pathogens, other infections that are caused by endoparasites such as Helminths (e.g., Schistosomiasis, Filariasis), as well as Protozoa (African sleeping sickness, Chagas’ disease, Leishmaniasis).In environments where NTDs prevail, Malaria, the most widespread disease caused by a “protozoan” endoparasite—although not currently treated as such by the WHO—can also be considered as a neglected disease.It is therefore a pleasure to invite high quality studies, as well as timely review papers, on biological activity, isolation and structure elucidation of natural and synthetic molecules, hit-to-lead development, lead optimization, investigations of the pharmacodynamics and -kinetics, as well as structure–activity relationships against diseases caused by endoparasites.As the editor, I cordially invite all participating scientists to publish their work related to the COST Action CM1307 in this Special Issue.They are termed “neglected” due to lack of financial investment into research and development of new drugs and almost non-existent public awareness in high-income countries.

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