| Literature DB >> 26367273 |
Massimo Bertinaria1, Pamela Orjuela-Sanchez2, Elisabetta Marini1, Stefano Guglielmo1, Anthony Hofer2, Yuri C Martins2, Graziela M Zanini3, John A Frangos2, Alberto Gasco1, Roberta Fruttero1, Leonardo J M Carvalho4.
Abstract
Hybrid products in which the dihydroartemisinin scaffold is combined with NO-donor furoxan and NONOate moieties have been synthesized and studied as potential tools for the treatment of cerebral malaria (CM). The designed products were able to dilate rat aorta strips precontracted with phenylephrine with a NO-dependent mechanism. All hybrid compounds showed preserved antiplasmodial activity in vitro and in vivo against Plasmodium berghei ANKA, comparable to artesunate and artemether. Hybrid 10, selected for additional studies, was capable of increasing survival of mice with late-stage CM from 27.5% to 51.6% compared with artemether. Artemisinin-NO-donor hybrid compounds show promise as potential new drugs for treating cerebral malaria.Entities:
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Year: 2015 PMID: 26367273 PMCID: PMC6003618 DOI: 10.1021/acs.jmedchem.5b01036
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446