| Literature DB >> 22512909 |
Theresa Dinio1, Alexander P Gorka, Andrew McGinniss, Paul D Roepe, Jeremy B Morgan.
Abstract
Plasmodium falciparum, the deadliest malarial parasite species, has developed resistance against nearly all man-made antimalarial drugs within the past century. However, quinine (QN), the first antimalarial drug, remains efficacious worldwide. Some chloroquine resistant (CQR) P. falciparum strains or isolates show mild cross resistance to QN, but many do not. Further optimization of QN may provide a well-tolerated therapy with improved activity versus CQR malaria. Thus, using the Heck reaction, we have pursued a structure-activity relationship study, including vinyl group modifications of QN. Certain derivatives show good antiplasmodial activity in QN-resistant and QN-sensitive strains, with lower IC(50) values relative to QN.Entities:
Mesh：
Substances：
Year: 2012 PMID： 22512909 PMCID： PMC3345081 DOI： 10.1016/j.bmc.2012.03.042
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641