Here we report the development of a straightforward synthetic procedure for the preparation of spirocyclic endoperoxides as synthetic analogues of the natural product dihydroplakortin. The peroxides presented here are more potent antiplasmodials than dihydroplakortin itself and we proved for the first time their antimalarial activity in vivo.
Synthetic spirocyclic endoperoxides : new antimalarial scaffolds / M. Brindisi, S. Gemma, S. Kunjir, L. Di Cerbo, S. Brogi, S. Parapini, S. D'Alessandro, D. Taramelli, A. Habluetzel, S. Tapanelli, S. Lamponi, E. Novellino, G. Campiani, S. Butini. - In: MEDCHEMCOMM. - ISSN 2040-2503. - 6:2(2015), pp. 357-362. [10.1039/C4MD00454J]
Synthetic spirocyclic endoperoxides : new antimalarial scaffolds
S. Parapini;S. D'Alessandro;D. Taramelli;
2015
Abstract
Here we report the development of a straightforward synthetic procedure for the preparation of spirocyclic endoperoxides as synthetic analogues of the natural product dihydroplakortin. The peroxides presented here are more potent antiplasmodials than dihydroplakortin itself and we proved for the first time their antimalarial activity in vivo.
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